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1
Almajali, Belal, Hamid Ali Nagi Al-Jamal, Wan Rohani Wan Taib, et al. "Thymoquinone, as a Novel Therapeutic Candidate of Cancers." Pharmaceuticals 14, no. 4 (2021): 369. http://dx.doi.org/10.3390/ph14040369.
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To date, natural products are widely used as pharmaceutical agents for many human diseases and cancers. One of the most popular natural products that have been studied for anticancer properties is thymoquinone (TQ). As a bioactive compound of Nigella sativa, TQ has shown anticancer activities through the inhibition of cell proliferation, migration, and invasion. The anticancer efficacy of TQ is being investigated in several human cancers such as pancreatic cancer, breast cancer, colon cancer, hepatic cancer, cervical cancer, and leukemia. Even though TQ induces apoptosis by regulating the expression of pro- apoptotic and anti-apoptotic genes in many cancers, the TQ effect mechanism on such cancers is not yet fully understood. Therefore, the present review has highlighted the TQ effect mechanisms on several signaling pathways and expression of tumor suppressor genes (TSG). Data from relevant published experimental articles on TQ from 2015 to June 2020 were selected by using Google Scholar and PubMed search engines. The present study investigated the effectiveness of TQ alone or in combination with other anticancer therapeutic agents, such as tyrosine kinase inhibitors on cancers, as a future anticancer therapy nominee by using nanotechnology.
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Blacquiere, Johanna M., Oana Sicora, Christopher M. Vogels, et al. "Dihydropyrimidinones containing boronic acids." Canadian Journal of Chemistry 83, no. 12 (2005): 2052–59. http://dx.doi.org/10.1139/v05-211.
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The addition of formylphenylboronic acid derivatives to urea and ethyl acetoacetate proceeds in the absence of an additional Lewis acid catalyst to give the corresponding dihydropyrimidinones (Biginelli products) in good yields. Novel boron-containing dihydropyrimidinones have been investigated for their ability to act as anticancer agents against the breast cancer cell line MCF7.Key words: anticancer, Biginelli compounds, boronic acids, breast cancer, dihydropyrimidinones.
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Ghanta, Venkata Rao, Nagaraju Madala, Aparna Pasula, et al. "Novel dermacozine-1-carboxamides as promising anticancer agents with tubulin polymerization inhibitory activity." RSC Advances 9, no. 32 (2019): 18670–77. http://dx.doi.org/10.1039/c9ra02416f.
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In the present study, novel dermacozine-1-carboxamides (8a–8n) were synthesized and screened for their in vitro cytotoxic activity against three different cancer cell lines: MCF-7 (breast cancer), A-549 (lung cancer) and DU145 (prostate cancer).
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Zhang, Ya-Zhou, Hai-Lin Liu, Qian-Song He, and Zhi Xu. "The In Vitro Anticancer Activity and Potential Mechanism of Action of 1-[(1R,2S)-2-fluorocyclopropyl]Ciprofloxacin-(4-methyl/phenyl/benzyl-3- aryl)-1,2,4-triazole-5(4H)-thione Hybrids." Current Topics in Medicinal Chemistry 20, no. 16 (2020): 1493–98. http://dx.doi.org/10.2174/1568026620666200310123723.
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Aims: Development of 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)- thione hybrids as potential dual-acting mechanism anticancer agent to overcome the drug resistance. Background: Chemotherapy is an essential tool for the treatment of lung and female breast cancers, and numerous anticancer agents have been launched for this purpose. However, the clinical outcomes of chemotherapy are usually far from satisfactory due to the side effects and resistance to chemotherapeutic drugs. Thus, it is urgent to develop novel anti-lung and anti-breast cancer agents. Background: Chemotherapy is an essential tool for the treatment of lung and female breast cancers, and numerous anticancer agents have been launched for this purpose. However, the clinical outcomes of chemotherapy are usually far from satisfactory due to the side effects and resistance to chemotherapeutic drugs. Thus, it is urgent to develop novel anti-lung and anti-breast cancer agents. Objective: The primary objective of this study was to evaluate the potential of bis-isatin scaffolds with alkyl/ether linkers between the two isatin moieties against different human breast cancer cell lines including A549, MCF-7 and their drug-resistant counterparts A549/CDDP, MCF-7/ADM cells. Methods: The 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin-(4-methyl/phenyl/benzyl-3-aryl)-1,2,4- triazole-5(4H)-thione hybrids were screened for their in vitro activity against drug-sensitive lung (A549), breast (MCF-7) and their drug-resistant counterparts A549/CDDP (cisplatin-resistant), MCF- 7/ADM (doxorubicin-resistant) cancer cell lines by MTT assay. The inhibitory activity of these hybrids against topoisomerase II and EGFR was also evaluated to investigate the potential mechanism of action of these hybrids. Result: The most prominent hybrid 7k (IC50: 37.28-49.05 µM) was comparable to Vorinostat against A549 and A549/CDDP lung cancer cells, and was 2.79-2.94 times more active than Vorinostat against MCF-7 and MCF-7/ADM breast cancer cell lines. Moreover, hybrid 7k (IC50: 8.6 and 16.4 µM) also demonstrated dual inhibition against topoisomerase II and EGFR. Conclusion: The 1-[(1R, 2S)-2-fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)-thione hybrids possess equally activity against both drug-sensitive cancer cells and their drug-resistant counterparts, and the majority of them were no inferior to the reference Vorinostat. The mechanistic study revealed that these hybrids could inhibit both topoisomerase II and EGFR, so these hybrids can be developed as dual-acting mechanism anticancer agents.
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Shaik, Afzal B., Yejella R. Prasad, Srinath Nissankararao, and Shaik Shahanaaz. "Synthesis, Biological and Computational Evaluation of Novel 2,3-dihydro-2-aryl-4-(4- isobutylphenyl)-1,5-benzothiazepine Derivatives as Anticancer and Anti-EGFR Tyrosine Kinase Agents." Anti-Cancer Agents in Medicinal Chemistry 20, no. 9 (2020): 1115–28. http://dx.doi.org/10.2174/1871520620666200130091142.
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Background: Despite the availability of a variety of chemotherapeutic agents, cancer is still one of the leading causes of death worldwide because of the problems with existing chemotherapeutic agents like objectionable side effects, lack of selectivity, and resistance. Hence, there is an urgent need for the development of novel anticancer agents with high usefulness, fewer side effects, devoid of resistance and superior selectivity. Objective: The objective of this study is to synthesize a series of novel 1,5-benzothiazepine derivatives and evaluate their anticancer activity employing biological and computational methods. Methods: Twenty new benzothiazepines (BT1-BT20) were prepared by condensing different 1-(4- isobutylphenyl)ethanone chalcones with 2-amiothiophenol and evaluated for their anticancer activity by MTT assay against three cell lines including HT-29 (colon cancer), MCF-7 (breast cancer) and DU-145 (prostate cancer). These compounds were also tested for their inhibitory action against EGFR (Epidermal Growth Factor Receptor) tyrosine kinase enzyme by taking into account of their excellent action against colon and breast cancer cell lines. Further, the structural features responsible for the activity were identified by Pharmacophorebased modelling using Schrodinger’s PHASETM software. Results: Among the 20 benzothiazepine derivatives, three compounds viz., BT18, BT19 and BT20 exhibited promising activity against the cell lines tested and the activity of BT20 was more than the standard methotrexate. Again the above three compounds showed excellent inhibitory activity with the percentage inhibition of 64.5, 57.3 and 55.8 respectively against EGFR (Epidermal Growth Factor Receptor) tyrosine kinase. PHASE identified a five-point AHHRR model for the proposed activity and the computational studies provided insights into the structural requirements for the anticancer activity and the results were consistent with the observed in vitro activity data. Conclusion: These novel benzothiazepines will be useful as lead molecules for the further development of new cancer therapies against colon and breast cancers.
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Abdelazeem, Ahmed H., Yasser M. A. Mohamed, Ahmed M. Gouda, Hany A. Omar, and Majed M. Al Robaian. "Novel Thymohydroquinone Derivatives as Potential Anticancer Agents: Design, Synthesis, and Biological Screening." Australian Journal of Chemistry 69, no. 11 (2016): 1277. http://dx.doi.org/10.1071/ch16102.
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The safety and efficacy of naturally occurring anticancer agents and their derivatives such as thymoquinone (TQ) and thymohydroquinone (THQ) have gained a rapidly growing interest. In an attempt to develop novel anticancer agents with superior activity, TQ was allowed to react with hydrazine hydrate, producing hydrazino thymohydroquinone 3. This new intermediate was subsequently reacted with various isocyanates, isothiocyanates, and acyl halides, affording three series of semicarbazone, semithiocarbazone, and acyl hydrazone derivatives, respectively. Subsequently, the anticancer activity of all the newly synthesised compounds against a panel of cancer cell lines was evaluated. Initial screening of the ability of the test compounds to inhibit cancer cell viability using the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay revealed that compounds 5d and 6 exerted better activity against breast cancer than TQ, with half-maximal inhibitory concentration (IC50) values of 9.6 and 10.0 μM, respectively. MTT results were confirmed by the ability of these compounds to elicit apoptotic cell death through the activation of caspase 3/7 enzymes. Together, the present work provided a novel class of THQ-based derivatives with potent anticancer and apoptosis properties, thereby warranting further optimisation of these derivatives as novel members in cancer treatment protocols.
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Anders, Carey K., Nicole R. LeBoeuf, Lara Bashoura, Saadia A. Faiz, Afreen I. Shariff, and Alexandra Thomas. "What’s the Price? Toxicities of Targeted Therapies in Breast Cancer Care." American Society of Clinical Oncology Educational Book, no. 40 (May 2020): 55–70. http://dx.doi.org/10.1200/edbk_279465.
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Agents with mechanisms novel to breast cancer care have been approved to treat breast cancer. These agents include drugs that target cyclin-dependent kinases, phosphoinositide 3-kinase PI3KCA gene mutations, PARP, checkpoint regulation, and novel antibody-drug conjugates. However, these novel approaches bring a risk of toxicities quite different from those of conventional cytotoxic chemotherapy. Here, we review these agents and discuss related adverse events, with particular attention to endocrine, pulmonary, and dermatologic toxicities. Endocrine toxicities associated with novel cancer therapies for breast cancer are distinct and often present with symptoms related to the specific hormonal deficiencies and rarely hormonal excess. Given the complex and sometimes irreversible nature of these toxicities, once recognized, transdisciplinary management with an endocrinologist experienced with managing drug-related toxicities is encouraged. Drug-related pneumonitis is a serious concern with new targeted therapies. Presentation may not be easily distinguished, and a multidisciplinary team approach can optimize patient care. Heightened awareness is crucial for early detection and treatment. Management should follow recommendations provided by the National Cancer Institute Common Terminology Criteria for Adverse Events and agent-specific guidelines. Cutaneous toxicities from anticancer therapies represent a common and often poorly characterized challenge for patients with breast cancer. Although our understanding of dermatologic effects from novel therapies continues to improve, the breadth of toxicities spans all dermatologic conditions. Targeted therapies offer effective and often novel therapeutic strategies for patients with breast cancer but also bring new adverse event profiles. In this era, it will be important both to closely follow monitoring recommendations and to remain vigilant for emerging toxicities.
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Ahsan, Mohamed Jawed, Jyotika Sharma, Monika Singh, Surender Singh Jadav, and Sabina Yasmin. "Synthesis and Anticancer Activity ofN-Aryl-5-substituted-1,3,4-oxadiazol-2-amine Analogues." BioMed Research International 2014 (2014): 1–9. http://dx.doi.org/10.1155/2014/814984.
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In continuance of our search for anticancer agents, we report herein the synthesis and anticancer activity of some novel oxadiazole analogues. The compounds were screened for anticancer activity as per National Cancer Institute (NCI US) protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers cell lines.N-(2,4-Dimethylphenyl)-5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-amine (4s) showed maximum activity with mean growth percent (GP) of 62.61 and was found to be the most sensitive on MDA-MB-435 (melanoma), K-562 (leukemia), T-47D (breast cancer), and HCT-15 (colon cancer) cell lines with GP of 15.43, 18.22, 34.27, and 39.77, respectively. Maximum GP was observed on MDA-MB-435 (melanoma) cell line (GP=6.82) by compoundN-(2,4-dimethylphenyl)-5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-amine (4u).
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Gaber, Ahmed, Walaa F. Alsanie, Deo Nandan Kumar, Moamen S. Refat, and Essa M. Saied. "Novel Papaverine Metal Complexes with Potential Anticancer Activities." Molecules 25, no. 22 (2020): 5447. http://dx.doi.org/10.3390/molecules25225447.
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Cancer is one of the leading causes of death worldwide. Although several potential therapeutic agents have been developed to efficiently treat cancer, some side effects can occur simultaneously. Papaverine, a non-narcotic opium alkaloid, is a potential anticancer drug that showed selective antitumor activity in various tumor cells. Recent studies have demonstrated that metal complexes improve the biological activity of the parent bioactive ligands. Based on those facts, herein we describe the synthesis of novel papaverine–vanadium(III), ruthenium(III) and gold(III) metal complexes aiming at enhancing the biological activity of papaverine drug. The structures of the synthesized complexes were characterized by various spectroscopic methods (IR, UV–Vis, NMR, TGA, XRD, SEM). The anticancer activity of synthesized metal complexes was evaluated in vitro against two types of cancer cell lines: human breast cancer MCF-7 cells and hepatocellular carcinoma HepG-2 cells. The results revealed that papaverine-Au(III) complex, among the synthesized complexes, possess potential antimicrobial and anticancer activities. Interestingly, the anticancer activity of papaverine–Au(III) complex against the examined cancer cell lines was higher than that of the papaverine alone, which indicates that Au-metal complexation improved the anticancer activity of the parent drug. Additionally, the Au complex showed anticancer activity against the breast cancer MCF-7 cells better than that of cisplatin. The biocompatibility experiments showed that Au complex is less toxic than the papaverine drug alone with IC50 ≈ 111 µg/mL. These results indicate that papaverine–Au(III) complex is a promising anticancer complex-drug which would make it a suitable candidate for further in vivo investigations.
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Alvarez, Ricardo H., Vicente Valero, and Gabriel N. Hortobagyi. "Emerging Targeted Therapies for Breast Cancer." Journal of Clinical Oncology 28, no. 20 (2010): 3366–79. http://dx.doi.org/10.1200/jco.2009.25.4011.
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Increased understanding of the molecular events involved in cancer development has led to the identification of a large number of novel targets and, in parallel, to the development of multiple approaches to anticancer therapy. Targeted therapy focuses on specific molecules in the malignant cell signal transduction machinery, including crucial molecules involved in cell invasion, metastasis, apoptosis, cell-cycle control, and tumor-related angiogenesis. In breast cancer, two new targeted agents have recently been approved: lapatinib, directed against the human epidermal growth factor receptor 2 (HER2); and bevacizumab, directed against vascular endothelial growth factor (VEGF). Multiple other targeted agents are under evaluation in clinical trials, including inhibitors of the epidermal growth factor receptor (EGFR), dual EGFR and HER2 inhibitors, other VEGF or VEGF-receptor inhibitors, and agents that alter crucial signaling pathways, such as RAS/MEK/ERK; phosphatidylinositol-3-kinase/Akt/ mammalian target of rapamycin; insulin-like growth factor/insulin-like growth factor receptor; poly (ADP-ribose) polymerase 1; and others. In this review, we present the most promising studies of these new targeted therapies and novel combinations of targeted therapies with traditional cytotoxic agents.
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Bhat, Mashooq Ahmad, M. Al-Tahhan, Mohamed A. Al-Omar, Ahmed M. Naglah, and Abdullah Al-Dhfyan. "Design and Synthesis of Novel Thiosemicarbazones as Potent Anti-breast Cancer Agents." Letters in Drug Design & Discovery 16, no. 4 (2019): 446–52. http://dx.doi.org/10.2174/1570180815666181008100944.
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Background: Thiosemicarbazones and its derivatives received a great pharmaceutical importance due to their prominent biological activities. Methods: A series of disubstituted thiosemicarbazone derivatives (1-12) were designed and synthesized as pure compounds in good yield. All the synthesized compounds were analyzed by spectral data. The anticancer activity of all the compounds was performed against breast cancer MCF-7 and MDA-MB-231 cell lines. Results: Most of the compounds showed activity against breast cancer MCF-7 and MDA-MB-231 cell lines with (IC50 = 12.25 µM ‒ 185.35 µM) and (IC50 = 12.97 µM ‒ 107.33 µM), respectively. Compound 9 presented (IC50 = 12.76 µM and 12.97 µM) against MCF-7 and MDA-MB-231 cell lines, respectively. Conclusion: Compound 9, was found to exhibit significant anti-breast cancer activity. This compound was further evaluated for side population percent inhibition assay on the breast cancer cell line MCF-7 at 5 and 10 µM concentration. It showed superiority to block side population by more than 80% at 5 μM concentration compared to the reference drug verapamil.
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Abdelazeem, Ahmed H., Yasser M. A. Mohamed, Ahmed M. Gouda, Hany A. Omar, and Majed M. Al Robaian. "Corrigendum to: Novel Thymohydroquinone Derivatives as Potential Anticancer Agents: Design, Synthesis, and Biological Screening." Australian Journal of Chemistry 70, no. 6 (2017): 755. http://dx.doi.org/10.1071/ch16102_co.
Full textAbstract:
The safety and efficacy of naturally occurring anticancer agents and their derivatives such as thymoquinone (TQ) and thymohydroquinone (THQ) have gained a rapidly growing interest. In an attempt to develop novel anticancer agents with superior activity, TQ was allowed to react with hydrazine hydrate, producing hydrazino thymohydroquinone 3. This new intermediate was subsequently reacted with various isocyanates, isothiocyanates, and acyl halides, affording three series of semicarbazone, semithiocarbazone, and acyl hydrazone derivatives, respectively. Subsequently, the anticancer activity of all the newly synthesised compounds against a panel of cancer cell lines was evaluated. Initial screening of the ability of the test compounds to inhibit cancer cell viability using the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay revealed that compounds 5d and 6 exerted better activity against breast cancer than TQ, with half-maximal inhibitory concentration (IC50) values of 9.6 and 10.0?M, respectively. MTT results were confirmed by the ability of these compounds to elicit apoptotic cell death through the activation of caspase 3/7 enzymes. Together, the present work provided a novel class of THQ-based derivatives with potent anticancer and apoptosis properties, thereby warranting further optimisation of these derivatives as novel members in cancer treatment protocols.
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Murti, Yogesh, and Pradeep Mishra. "Synthesis, Characterization, and Biological Evaluation of Novel Naringenin Derivatives as Anticancer Agents." Current Bioactive Compounds 16, no. 4 (2020): 442–48. http://dx.doi.org/10.2174/1573407215666181214114927.
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Background: In the present study, a series of substituted naringenin derivatives was synthesized by Claisen–Schmidt reaction using grinding technique. Methods: Synthesized compounds were characterized on the basis of Fourier-Transform Infrared Spectroscopy (FTIR), proton Nuclear Magnetic Resonance (1H NMR), Mass Spectroscopy (MS) and elemental analysis. These derivatives were screened for anticancer activity on breast (MCF-7) and colon (HT-29) cell lines using Sulforhodamine B (SRB) colorimetric assay. Results: Results displayed improved inhibitory concentration (IC50) values of naringenin derivatives. IC50 values of 3(4-chlorobenzylidene)-5,7-dihydroxy-2(4-hydroxyphenyl)chroman-4-one are 10.35 μM (MCF-7) & 12.03 μM (HT-29), which is most potent compound in the series. These finding confirms the suitability of 3-substituted naringenin in improving the anticancer effect. Conclusion: Due to the intense interest in the development of drugs capable of inhibiting cancerous cells, naringenin derivatives may represent important precursor molecules for the therapeutic armamentarium of colon and breast cancer. Further structural modification in these structures will be of interest and may result in compounds having a better anticancer activity.
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Naresh, Vema Venkata, Y. Bharathi Kumari, Mussulla Sridhar, Addada Ramakrishnam Raju, and A. Srinivasa Rao. "Synthesis and Biological Evaluation of 1,3,4-Oxadiazole Fused Resveratrol Derivatives as Anticancer Agents." Asian Journal of Chemistry 32, no. 8 (2020): 1967–71. http://dx.doi.org/10.14233/ajchem.2020.22680.
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A novel target compounds (9a-j) were design and synthesized and characterized by 1H & 13C NMR, ESI-MS spectral analysis. Further, these were tested for their anticancer activity against three human cancer cell lines such as MCF-7, MDA MB-231 (breast), A549 (Lung) and adriamycin was used as positive control. Among ten compounds, two compounds like 9b and 9j were showed a significant anticancer activity compared to control drug.
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Pappachen, Leena K., Subin Mary Zachariah, and Deepthy Chandran. "INSILICO DESIGN, SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL BENZOTHIAZOLE DERIVATIVES AS ANTI-CANCER AGENTS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 4 (2017): 150. http://dx.doi.org/10.22159/ajpcr.2017.v10i4.16407.
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Objectives: Cancer is a disease characterized by uncontrollable, irreversible, independent, autonomous, uncoordinated and relatively unlimited and abnormal over growth of tissues. Breast cancer is the second most common type of cancer after lung cancer. The aim of the study is to carry out the docking studies, synthesis and anti-tumour activities of Benzothiazole derivatives containing oxadiazole groups or amino groups.Methods: The docking studies of benzothiazole derivatives were done with known anti-cancer targets like oestrogen receptor by using argus lab and auto dock programmes with the standard drug tamoxifen. Based upon the results obtained from the molecular modeling, the derivatives were selected for the synthesis. The synthesized compounds were characterized by melting point, TLC, IR, 1H NMR, 13CNMR, MASS spectral data and screened for their in- vitro anti-cancer activities.Results: The docking scores obtained for benzothiazole derivatives (BT1,BT2,BT3,BT4) and std.tamoxifen from the preliminary docking program by using argusLab were- 9.68,-9.4,-9.59, -11.1988,-9.71 and by using autodock program were -6.29, -5.25,-7.19,-7.48,-3.86 respectively. All the four derivatives were synthesized, characterized and subjected to in vitro anticancer screening by MTT assay in breast cancer (MCF-7) cell lines. Compounds DBT1, DBT2, DBT3 were the most active compounds against MCF-7 cell lines with IC50 of 70.0, 64.0 and 65.0, respectively.Conclusion: All the four derivatives show good docking scores when compared to standard drug and can be concluded that all the synthesized benzothiazole ligands show good anti-cancer property.Keywords: Benzothiazole, Oxadiazole, Estrogen receptor, Anticancer targets.
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Al Zahrani, Nourah A., Reda M. El-Shishtawy, Mahmoud M. Elaasser, and Abdullah M. Asiri. "Synthesis of Novel Chalcone-Based Phenothiazine Derivatives as Antioxidant and Anticancer Agents." Molecules 25, no. 19 (2020): 4566. http://dx.doi.org/10.3390/molecules25194566.
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Based on reported results for the potential medicinal impact of phenothiazine core, as well as the chalcone skeleton that is widely present in many natural products, together with their reported bioactivities, the present work was aimed at combining both moieties in one molecular skeleton and to synthesize and characterize a novel series of chalone-based phenothiazine derivatives. For this purpose, 2-acetylphenothiazine was N-alkylated, followed by the Claisen-Schmidt reaction to produce the chalcones with good yield. Antioxidant activity, as evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, was assessed to determine if their antioxidant potential was comparable with ascorbic acid, and attributable to the phenothiazine core. Screening anticancer activities of the synthesized chalone-based phenothiazine derivatives against human breast cancer cell line MCF-7 cells, and human hepatocellular carcinoma HepG-2 cells, compared with standard drugs cisplatin and doxorubicin, was evaluated. The results revealed that compounds 4a, 4b, 4d, 4h, 4j, 4k, 4m, 4o, and 4p were good against human hepatocellular carcinoma HepG-2 cells, and among these compounds 4b and 4k were the most effective compounds, with IC50 values of 7.14 μg/mL and 7.6 1 μg/mL, respectively. On the other hand, compounds 4a, 4b, 4k, and 4m were good against human breast cancer cell line MCF-7 cells and, among these compounds, 4k and 4b were the most effective compounds, with IC50 values of 12 μg/mL and 13. 8 μg/mL, respectively. The overall results suggest that these compounds could, potentially, be further modified for the formation of more potent antioxidant and anticancer agents.
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Yang, Mingli, Hailin Liu, Yazhou Zhang, Xiujun Wang, and Zhi Xu. "Moxifloxacin-isatin Hybrids Tethered by 1,2,3-triazole and their Anticancer Activities." Current Topics in Medicinal Chemistry 20, no. 16 (2020): 1461–67. http://dx.doi.org/10.2174/1568026620666200128144825.
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Aims: To explore more active fluoroquinolone anticancer candidates. Background: Cancer which can affect almost any part of the body, is most striking and deadliest disease. It is estimated that around one in five people globally develop cancer during their lifetime, and approximately 10% people eventually die from this disease, and 18.1 million new cancer cases with 9.6 million deaths occurred in 2018. The anticancer agents play an intriguingly role in fighting against cancer, and above 100 drugs have already been marketed for this purpose. However, the major drawback of current accessible anticancer agents is the low specificity which results in many side effects. Moreover, cancer cells have already generated resistance to almost all available drugs, creating an urgent need to novel anticancer agents with high specificity and great efficiency especially towards drug-resistant cancers. Quinolone and isatin derivatives were reported to possess promising anticancer activity, high specificity, and relatively few side effects. Currently, several quinolone and isatin derivatives such as Voreloxin, Quarfloxin, AT-3639, Semaxanib, Sunitinib and Nintedanib have already been introduced in clinical practice or under evaluations for the treatment of cancer including drug-resistant cancers, revealing their potential as novel anticancer agents. Hybrid molecules have the potential to increase the specificity, improve the efficiency, and overcome the drug resistance, so hybridization is a promising strategy in the drug discovery. Some of the moxifloxacin-isatin hybrids exhibited considerable activity against various cancer cells even drug-resistant cells, so it is conceivable that hybridization of quinolone and isatin moieties may provide novel anticancer candidates. The structure-activity relationships (SARs) demonstrated that the linkers between quinolone and isatin skeletons were critical for the biological activity, and 1,2,3-triazole could exert various noncovalent interactions with biological targets, so introduction of 1,2,3-triazole as the linker between the two moieties may provide more efficient anticancer candidates. Objective: To explore more active fluoroquinolone anticancer candidates and enrich the structureactivity relationships of fluoroquinolone-isatin hybrids. Methods: The synthesized moxifloxacin-isatin hybrids 5a-c, 6a-g and 13a-d were assessed for their anticancer activities against liver cancer cells HepG2, breast cancer cells MCF-7, MCF-7/DOX, prostate cancer cells DU-145 and MDR DU-145 by MTT assay. Hybrid 5b was selected for further evaluation of its tubulin polymerization inhibitory activity with combretastatin A-4 as comparison. Results: Most of the synthesized hybrids were active against the tested cancer cell lines, and the most active hybrid 5b (IC50: 31.3-76.8 μM) was more potent than vorinostat (IC50: 96.7->100 μM), demonstrating moxifloxacin-isatin hybrids are potential anticancer candidates. Conclusion: The mechanism study revealed that inhibition of tubulin polymerization is at least one of the mechanisms of action for this kind of hybrids. Other: The structure-activity relationship was summarized for further rational design of more efficient anticancer candidates.
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Ramalingeswara Rao, B., Mohana Rao Katiki, Dileep Kommula, SaiShyam Narayanan, Ruby John Anto, and M. S. R. Murty. "Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents." Croatica chemica acta 92, no. 3 (2019): 393–402. http://dx.doi.org/10.5562/cca3535.
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The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 µM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.
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Ielo, Ileana, Domenico Iacopetta, Carmela Saturnino, et al. "Gold Derivatives Development as Prospective Anticancer Drugs for Breast Cancer Treatment." Applied Sciences 11, no. 5 (2021): 2089. http://dx.doi.org/10.3390/app11052089.
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Commonly used anticancer drugs are cisplatin and other platinum-based drugs. However, the use of these drugs in chemotherapy causes numerous side effects and the onset of frequent drug resistance phenomena. This review summarizes the most recent results on the gold derivatives used for their significant inhibitory effects on the in vitro proliferation of breast cancer cell models and for the consequences deriving from morphological changes in the same cells. In particular, the study discusses the antitumor activity of gold nanoparticles, gold (I) and (III) compounds, gold complexes and carbene-based gold complexes, compared with cisplatin. The results of screening studies of cytotoxicity and antitumor activity for the gold derivatives show that the death of cancer cells can occur intrinsically by apoptosis. Recent research has shown that gold (III) compounds with square planar geometries, such as that of cisplatin, can intercalate the DNA and provide novel anticancer agents. The gold derivatives described can make an important contribution to expanding the knowledge of medicinal bioorganometallic chemistry and broadening the range of anticancer agents available, offering improved characteristics, such as increased activity and/or selectivity, and paving the way for further discoveries and applications.
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CSONKA, ANDREA, ANNAMÁRIA KINCSES, MÁRTA NOVÉ, et al. "Selenoesters and Selenoanhydrides as Novel Agents Against Resistant Breast Cancer." Anticancer Research 39, no. 7 (2019): 3777–83. http://dx.doi.org/10.21873/anticanres.13526.
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Singh, Namrata, Poonam Kushwaha, Amresh Gupta, and Om Prakash. "Recent Advances of Novel Therapeutic Agents from Botanicals for Prevention and Therapy of Breast Cancer: An Updated Review." Current Cancer Therapy Reviews 16, no. 1 (2020): 5–18. http://dx.doi.org/10.2174/1573394715666181129101502.
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Breast cancer is among the foremost common malignancies and the second leading cause for cancer-related deaths in females. Varied treatment approaches are projected to cause a subject matter reduction in the fatality rate. Carcinoma treatment is highly challenging due to therapeutic resistance and reoccurrence. Several studies have revealed that bioactive compounds isolated from natural products such as plants, vegetables, and marine origins have a therapeutic and preventive role in breast carcinoma. Utilization of these bioactive agents in amelioration of cancer as complementary and alternative therapy increases day by day due to growing scientific shreds of evidence of the biomedical innovation and clinical trials. Due to the safe nature of these photochemical investigators are focusing on the investigation of lead compounds from traditional herbal medicine to discover new lead anticancer agents in the single pure compound. This review highlights the mechanism of action and future prospects of novel medicinal agents from botanical sources that have chemoprevention activity against breast carcinoma together with other types of body cancer. The major bioactive, which are used as a remedy for the prevention and treatment of breast cancer, is summarized and explored here.
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Dube, Pritam N., Nikhil S. Sakle, Sachin A. Dhawale, Shweta A. More, and Santosh N. Mokale. "Synthesis, Biological Investigation and Docking Study of Novel Chromen Derivatives as Anti-Cancer Agents." Anti-Cancer Agents in Medicinal Chemistry 19, no. 9 (2019): 1150–60. http://dx.doi.org/10.2174/1871520619666190307121145.
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Background: According to the latest global cancer data, cancer burden rises to 18.1 million new cases and 9.6 million cancer deaths in 2018. Among that female breast cancer ranks as the fifth leading cause of death (627000 deaths, 6.6%). The main causative factor involved in breast cancer development and progression is the Estrogen Receptor (ER) which is the essential target for anti-cancer drug discovery. Since millennia ER-α has been considered as an oncology mark for the treatment of breast cancer. Methods: A series of novel 6-methyl-3-(3-oxo-1-phenyl-3-(4-(2-(piperidin-1-yl)ethoxy)phenyl)propyl)-2Hchromen- 2-one was designed, synthesized and screened for their anti-breast cancer activity against estrogen receptor-positive MCF-7, ZR-75-1 and negative MDA-MB-435 human breast cancer cell lines. Estrogen level of all the potent cytotoxic compounds were measured on day 30 of intoxication was compared with the control and N-methyl-N-nitrosourea (MNU) group. The docking study was performed to predict binding orientation towards the estrogen receptor-α. Results: Among the synthesized compounds C-3, C-5 and C-15 were showing potent cytotoxicity against estrogen receptor-positive MCF-7. The potent cytotoxic compounds C-3, C-5 and C-15 were further evaluated for in vivo anti-cancer activity by MNU induced mammary carcinoma in female sprague-dawley rats. The in vivo anticancer activity result shows that the compound C-5 has protuberant affinity towards estrogen receptor as standard TAM (Tamoxifen). The docking of the synthesized chromen derivatives showed interaction modes comparable to that of the co-crystallized ligands. Conclusion: The designed class has very promising starting point for the development and further improvement in anti-breast cancer class of drugs.
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Tylińska, Beata, Benita Wiatrak, Żaneta Czyżnikowska, Aneta Cieśla-Niechwiadowicz, Elżbieta Gębarowska, and Anna Janicka-Kłos. "Novel Pyrimidine Derivatives as Potential Anticancer Agents: Synthesis, Biological Evaluation and Molecular Docking Study." International Journal of Molecular Sciences 22, no. 8 (2021): 3825. http://dx.doi.org/10.3390/ijms22083825.
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In the present paper, new pyrimidine derivatives were designed, synthesized and analyzed in terms of their anticancer properties. The tested compounds were evaluated in vitro for their antitumor activity. The cytotoxic effect on normal human dermal fibroblasts (NHDF) was also determined. According to the results, all the tested compounds exhibited inhibitory activity on the proliferation of all lines of cancer cells (colon adenocarcinoma (LoVo), resistant colon adenocarcinoma (LoVo/DX), breast cancer (MCF-7), lung cancer (A549), cervical cancer (HeLa), human leukemic lymphoblasts (CCRF-CEM) and human monocytic (THP-1)). In particular, their feature stronger influence on the activity of P-glycoprotein of cell cultures resistant to doxorubicin than doxorubicin. Tested compounds have more lipophilic character than doxorubicin, which determines their affinity for the molecular target and passive transport through biological membranes. Moreover, the inhibitory potential against topoisomerase II and DNA intercalating properties of synthesized compounds were analyzed via molecular docking.
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Duncan, R., M. J. Vicent, F. Greco, and R. I. Nicholson. "Polymer–drug conjugates: towards a novel approach for the treatment of endrocine-related cancer." Endocrine-Related Cancer 12, Supplement_1 (2005): S189—S199. http://dx.doi.org/10.1677/erc.1.01045.
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The last decade has seen successful clinical application of polymer–protein conjugates (e.g. Oncaspar, Neulasta) and promising results in clinical trials with polymer–anticancer drug conjugates. This, together with the realisation that nanomedicines may play an important future role in cancer diagnosis and treatment, has increased interest in this emerging field. More than 10 anticancer conjugates have now entered clinical development. Phase I/II clinical trials involving N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-doxorubicin (PK1; FCE28068) showed a four- to fivefold reduction in anthracycline-related toxicity, and, despite cumulative doses up to 1680 mg/m2 (doxorubicin equivalent), no cardiotoxicity was observed. Antitumour activity in chemotherapy-resistant/refractory patients (including breast cancer) was also seen at doxorubicin doses of 80–320 mg/m2, consistent with tumour targeting by the enhanced permeability (EPR) effect. Hints, preclinical and clinical, that polymer anthracycline conjugation can bypass multidrug resistance (MDR) reinforce our hope that polymer drugs will prove useful in improving treatment of endocrine-related cancers. These promising early clinical results open the possibility of using the water-soluble polymers as platforms for delivery of a cocktail of pendant drugs. In particular, we have recently described the first conjugates to combine endocrine therapy and chemotherapy. Their markedly enhanced in vitro activity encourages further development of such novel, polymer-based combination therapies. This review briefly describes the current status of polymer therapeutics as anticancer agents, and discusses the opportunities for design of second-generation, polymer-based combination therapy, including the cocktail of agents that will be needed to treat resistant metastatic cancer.
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Khanusiya, Mahammadali M., and Zakirhusen M. Gadhawala. "Synthesis and Biological Evaluation of Chalcones Possessing Ring Activating Groups as Potent of Anticancer Agents." International Letters of Chemistry, Physics and Astronomy 73 (April 2017): 1–8. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.73.1.
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Some novel anticancer agents based on chalcone scaffold were synthesized with potential therapeutic application for many types of cancer. Hydroxy and methoxy substitution on aryl ring of chalcone, depending upon positions in aryl ring influence anticancer and other activities. These chalcone molecules were evaluated for their invitro cytotoxic activity against five cancer cell lines including human chronic myelogenus-leukemia K-562, human breast adenocarcinoma MCF-7, human prostate carcinoma DU-145, human lung adenocarcinoma A-549 and normal VERO cell line. Most of the compounds being active cytotoxic agents and were shown to be non-toxic to normal cells. The synthesized compounds were characterized by means of their FT-IR, MASS and 1HNMR spectral study.
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Shindikar, Amol, Akshita Singh, Malcolm Nobre, and Saurabh Kirolikar. "Curcumin and Resveratrol as Promising Natural Remedies with Nanomedicine Approach for the Effective Treatment of Triple Negative Breast Cancer." Journal of Oncology 2016 (2016): 1–13. http://dx.doi.org/10.1155/2016/9750785.
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Researchers have made considerable progress in last few decades in understanding mechanisms underlying pathogenesis of breast cancer, its phenotypes, its molecular and genetic changes, its physiology, and its prognosis. This has allowed us to identify specific targets and design appropriate chemical entities for effective treatment of most breast cancer phenotypes, resulting in increased patient survivability. Unfortunately, these strategies have been largely ineffective in the treatment of triple negative breast cancer (TNBC). Hormonal receptors lacking render the conventional breast cancer drugs redundant, forcing scientists to identify novel targets for treatment of TNBC. Two natural compounds, curcumin and resveratrol, have been widely reported to have anticancer properties.In vitroandin vivostudies show promising results, though their effectiveness in clinical settings has been less than satisfactory, owing to their feeble pharmacokinetics. Here we discuss these naturally occurring compounds, their mechanism as anticancer agents, their shortcomings in translational research, and possible methodology to improve their pharmacokinetics/pharmacodynamics with advanced drug delivery systems.
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Aliwaini, Saeb, Bassam Abu Thaher, Ihab Al-Masri, et al. "Design, Synthesis and Biological Evaluation of Novel Pyrazolo[1,2,4]triazolopyrimidine Derivatives as Potential Anticancer Agents." Molecules 26, no. 13 (2021): 4065. http://dx.doi.org/10.3390/molecules26134065.
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Three novel pyrazolo-[4,3-e][1,2,4]triazolopyrimidine derivatives (1, 2, and 3) were designed, synthesized, and evaluated for their in vitro biological activity. All three compounds exhibited different levels of cytotoxicity against cervical and breast cancer cell lines. However, compound 1 showed the best antiproliferative activity against all tested tumor cell lines, including HCC1937 and HeLa cells, which express high levels of wild-type epidermal growth factor receptor (EGFR). Western blot analyses demonstrated that compound 1 inhibited the activation of EGFR, protein kinase B (Akt), and extracellular signal-regulated kinase (Erk)1/2 in breast and cervical cancer cells at concentrations of 7 and 11 µM, respectively. The results from docking experiments with EGFR suggested the binding of compound 1 at the ATP binding site of EGFR. Furthermore, the crystal structure of compound 3 (7-(4-bromophenyl)-9-(pyridin-4-yl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine) was determined by single crystal X-ray analysis. Our work represents a promising starting point for the development of a new series of compounds targeting EGFR.
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Kandeel, Manal M., Aliaa M. Kamal, Bassem H. Naguib, and Marwa S. A. Hassan. "Design, Synthesis, Cytotoxic Activity and Apoptosis-inducing Action of Novel Cinnoline Derivatives as Anticancer Agents." Anti-Cancer Agents in Medicinal Chemistry 18, no. 8 (2018): 1208–17. http://dx.doi.org/10.2174/1871520618666180220121319.
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Aims: Tyrosine kinases and topoisomerase I are common target enzymes for the majority of the anticancer agents. In contrast to quinazolines and quinolines, kinase inhibitors and topoisomerase inhibitors incorporating cinnoline scaffold are relatively infrequent. Thus the aim of this work was to replace the former scaffolds with the latter one. Eighteen novel cinnoline derivatives were designed, synthesized and characterized using both microanalytical and spectral data. Methods: The cytotoxic activity of the new compounds was screened in vitro against both human breast cancer cells and normal breast cells. Results: The enzymatic inhibition activity of promising candidates against both epidermal growth factor receptor tyrosine kinase and topoisomerase I was accomplished. Conclusions: Cell cycle profiles were observed at IC50 doses of representative biologically active compounds. Compound 7 represented a new scaffold incorporating triazepinocinnoline ring system and showed outstanding cytotoxic activity against MCF-7 (0.049 µM), tyrosine kinase inhibition (0.22 µM), apoptosis percentage and the highest selectivity index.
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Faustino, Célia, Íris Neto, Pedro Fonte, and Ana Macedo. "Cytotoxicity and Chemotherapeutic Potential of Natural Rosin Abietane Diterpenoids and their Synthetic Derivatives." Current Pharmaceutical Design 24, no. 36 (2019): 4362–75. http://dx.doi.org/10.2174/1381612825666190112162817.
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Cancer is a major cause of morbidity and mortality worldwide. Chemotherapeutic agents currently used in cancer treatment are associated with severe side effects and development of resistance. Thus, there is a pressing need for novel and more potent anticancer drugs with high selectivity for tumor cells and reduced toxicity to normal tissue. Natural products remain an important source of bioactive compounds and drug prototypes that can lead to new and more effective antitumor agents. Coniferous plants are rich in abietane diterpenoids with a wide range of biological activities that provide useful templates for synthetic modification. Abietic acid and dehydroabietic acid (DHA), the major diterpenic resin acids from Pinus rosin, and dehydroabietylamine found in commercial disproportionated rosin amine, display antibacterial and antitumor properties. These compounds and their synthetic derivatives have been reported as promising anticancer agents with potent growth inhibitory activity against several types of human cancer cell lines, including breast, ovarian, prostate, colon, liver, lung and cervical carcinoma cells. Their mechanisms of action are diverse and include DNA binding, induction of apoptosis or oncosis, tubulin polymerization inhibition and disruption of intracellular cholesterol transport. This review covers the main aspects of natural rosin abietane diterpenoids (abietic acid, DHA and DHAA) and synthetic derivatives concerning their anti-proliferative, cytotoxic and antitumor activities, mechanisms of action and structure- activity relationships relevant for the development of novel anticancer agents for cancer chemotherapy.
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Bak, Dong-ho, Seong Hee Kang, Chul-hong Park, Byung Yeoup Chung, and Hyoung-Woo Bai. "A novel radiolytic rotenone derivative, rotenoisin A, displays potent anticarcinogenic activity in breast cancer cells." Journal of Radiation Research 62, no. 2 (2021): 249–58. http://dx.doi.org/10.1093/jrr/rrab005.
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Abstract Chemotherapy for cancer treatment has therapeutic limitations, such as drug resistance, excessive toxic effects and undesirable adverse effects. Therefore, efforts to improve the safety and efficacy of chemotherapeutic agents are essential. Ionizing radiation can improve physiological and pharmacological properties by transforming structural modifications of the drug. In this study, in order to reduce the adverse effects of rotenone and increase anticancer activity, a new radiolytic rotenone derivative called rotenoisin A was generated through radiolytic transformation. Our findings showed that rotenoisin A inhibited the proliferation of breast cancer cells and increased the rate of apoptosis, whereas it had no inhibitory effect on primary epidermal keratinocytes compared with rotenone. Moreover, rotenoisin A-induced DNA damage by increasing reactive oxygen species (ROS) accumulation. It was also confirmed not only to alter the composition ratio of mitochondrial proteins, but also to result in structural and functional changes. The anticancer effect and molecular signalling mechanisms of rotenoisin A were consistent with those of rotenone, as previously reported. Our study suggests that radiolytic transformation of highly toxic compounds may be an alternative strategy for maintaining anticancer effects and reducing the toxicity of the parent compound.
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Izevbigie, Ernest B. "Discovery of Water-Soluble Anticancer Agents (Edotides) from a Vegetable Found in Benin City, Nigeria." Experimental Biology and Medicine 228, no. 3 (2003): 293–98. http://dx.doi.org/10.1177/153537020322800308.
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Cancer claims the lives of more than six million people each year in the world. About 1,268,000 new cancer cases, and 553,400 deaths were reported in the United States in 2001. Current treatment approaches have yielded significant progress in the fight against cancer, but the incidence of developing certain types of cancer continues to rise. This is especially true in the African-American communities. African Americans are about 33% more likely to die of cancer than are whites and more than twice likely to die of cancer as are Asian-Islander, American-Indians, and Hispanics. This increase coupled with the harsh side effects of some of the cancer chemotherapies have led to the search for more natural biological products, especially those derived from plant products, currently known as herbal medicine. There is a need for a continued search for novel natural products that may be used as cancer chemopreventive and/or chemotherapeutic agents. The objective of this study was to evaluate the effect(s) of a novel water-soluble leaf extract of Vernonia amygdalina (VA) on human breast cancer cell DNA synthesis. MCF-7 cell line, considered a suitable model, was used in this study. Treatment of cells with physiologically relevant concentrations of water-soluble VA extract potently inhibited DNA synthesis in a concentration-dependent fashion both in the absence and presence of serum. Fractions of VA extract separated using preparative reverse-phase chromatography also inhibited DNA synthesis (P < 0.005). These results suggest that VA vegetable, if incorporated in the diet, may prevent or delay the on-set of breast cancer.
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Abdallah, Amira E. M., Rafat M. Mohareb, Maher H. E. Helal, and Germeen J. Mofeed. "Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine." Acta Chimica Slovenica 68, no. 3 (2021): 604–16. http://dx.doi.org/10.17344/acsi.2020.6446.
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Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.
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Islam, Mohammad Shahidul, M. Ali, Abdullah Mohammed Al-Majid, et al. "Bimetallic Iron–Palladium Catalyst System as a Lewis-Acid for the Synthesis of Novel Pharmacophores Based Indole Scaffold as Anticancer Agents." Molecules 26, no. 8 (2021): 2212. http://dx.doi.org/10.3390/molecules26082212.
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The Friedel–Crafts reaction between substituted indoles as nucleophiles with chalcones-based benzofuran and benzothiophene scaffolds was carried out by employing a highly efficient bimetallic iron–palladium catalyst system. This catalytic approach produced the desired bis-heteroaryl products with low catalyst loading, a simple procedure, and with acceptable yield. All synthesized indole scaffolds 3a–3s were initially evaluated for their cytotoxic effect against human fibroblast BJ cell lines and appeared to be non-cytotoxic. All non-cytotoxic compounds 3a–3s were then evaluated for their anticancer activities against cervical cancer HeLa, prostate cancer PC3, and breast cancer MCF-7 cell lines, in comparison to standard drug doxorubicin, with IC50 values 1.9 ± 0.4 µM, 0.9 ± 0.14 µM and 0.79 ± 0.05 µM, respectively, and appeared to be moderate to weak anticancer agents. Fluoro-substituted chalcone moiety-containing compounds, 3b appeared to be the most active member of the series against cervical HeLa (IC50 = 8.2 ± 0.2 µM) and breast MCF-7 cancer cell line (IC50 = 12.3 ± 0.04 µM), whereas 6-fluroindol-4-bromophenyl chalcone-containing compound 3e (IC50 = 7.8 ± 0.4 µM) appeared to be more active against PC3 prostate cancer cell line.
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Yao, Chun-Hsu, Tsung-Chih Hsieh, Jen-Shin Song та Jinq-Chyi Lee. "Design, synthesis and anticancer evaluation of β-carboline-1-one hydantoins". Future Medicinal Chemistry 12, № 3 (2020): 183–92. http://dx.doi.org/10.4155/fmc-2019-0276.
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Aim: Cancer is a major health burden and a leading cause of death worldwide. We sought to discover potential anticancer molecules with novel scaffold for further development of more active agents to address the issue. Methodology: A series of β-carboline-1-one hydantoins were designed according to a conformational restriction strategy, synthesized via a one-pot Knoevenagel condensation−intramolecular cyclization, and tested in cytotoxicity assays. Results: The study culminated in the identification of 6b and 6c, both of which were found to potently inhibit breast and lung cancer cell lines. Of particular interest was 6c, which was 83 times more potent an inhibitor than 5-fluorouracil in inhibiting MCF-7. Conclusion: This work establishes β-carboline-1-one hydantoin as a promising scaffold in the investigation of anticancer agents.
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Ferraro, Maria Grazia, Marialuisa Piccolo, Gabriella Misso, et al. "Breast Cancer Chemotherapeutic Options: A General Overview on the Preclinical Validation of a Multi-Target Ruthenium(III) Complex Lodged in Nucleolipid Nanosystems." Cells 9, no. 6 (2020): 1412. http://dx.doi.org/10.3390/cells9061412.
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In this review we have showcased the preclinical development of original amphiphilic nanomaterials designed for ruthenium-based anticancer treatments, to be placed within the current metallodrugs approach leading over the past decade to advanced multitarget agents endowed with limited toxicity and resistance. This strategy could allow for new options for breast cancer (BC) interventions, including the triple-negative subtype (TNBC) with poor therapeutic alternatives. BC is currently the second most widespread cancer and the primary cause of cancer death in women. Hence, the availability of novel chemotherapeutic weapons is a basic requirement to fight BC subtypes. Anticancer drugs based on ruthenium are among the most explored and advanced next-generation metallotherapeutics, with NAMI-A and KP1019 as two iconic ruthenium complexes having undergone clinical trials. In addition, many nanomaterial Ru complexes have been recently conceived and developed into anticancer drugs demonstrating attractive properties. In this field, we focused on the evaluation of a Ru(III) complex—named AziRu—incorporated into a suite of both zwitterionic and cationic nucleolipid nanosystems, which proved to be very effective for the in vivo targeting of breast cancer cells (BBC). Mechanisms of action have been widely explored in the context of preclinical evaluations in vitro, highlighting a multitarget action on cell death pathways which are typically deregulated in neoplasms onset and progression. Moreover, being AziRu inspired by the well-known NAMI-A complex, information on non-nanostructured Ru-based anticancer agents have been included in a precise manner.
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Balogun, Toheeb A., Kaosarat D. Buliaminu, Onyeka S. Chukwudozie, Zainab A. Tiamiyu, and Taiwo J. Idowu. "Anticancer Potential of Moringa oleifera on BRCA-1 Gene: Systems Biology." Bioinformatics and Biology Insights 15 (January 2021): 117793222110107. http://dx.doi.org/10.1177/11779322211010703.
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Breast cancer has consistently been a global challenge that is prevalent among women. There is a continuous increase in the high number of women mortality rates because of breast cancer and affecting nations at all modernization levels. Women with high-risk factors, including hereditary, obesity, and menopause, have the possibility of developing breast cancer growth. With the advent of radiotherapy, chemotherapy, hormone therapy, and surgery in breast cancer treatment, breast cancer survivors have increased. Also, the design and development of drugs targeting therapeutic enzymes effectively treat the tumour cells early. However, long-term use of anticancer drugs has been linked to severe side effects. This research aims to develop potential drug candidates from Moringa oleifera, which could serve as anticancer agents. In silico analysis using Schrödinger Molecular Drug Discovery Suite and SWISS ADME was employed to determine the therapeutic potential of phytochemicals from M oleifera against breast cancer via molecular docking, pharmacokinetic parameters, and drug-like properties. The result shows that rutin, vicenin-2, and quercetin-3-O-glucoside have the highest binding energy of −7.522, −6.808, and −6.635 kcal/mol, respectively, in the active site of BRCA-1. The essential amino acids involved in the protein-ligand interaction following active site analysis are ASN 1678, ASN 1774, GLY 1656, LEU 1657, GLN 1779, LYS 1702, SER 1655, PHE 1662, ARG 1699, GLU 1698, and VAL 1654. Thus, we propose that bioactive compounds from M oleifera may be potential novel drug candidates in the treatment of breast cancer.
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Rani, Priyanka, Dilipkumar Pal, Rahul Rama Hegde, and Syed Riaz Hashim. "Anticancer, Anti-Inflammatory, and Analgesic Activities of Synthesized 2-(Substituted phenoxy) Acetamide Derivatives." BioMed Research International 2014 (2014): 1–9. http://dx.doi.org/10.1155/2014/386473.
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The aphorism was to develop new chemical entities as potential anticancer, anti-inflammatory, and analgesic agents. The Leuckart synthetic pathway was utilized in development of novel series of 2-(substituted phenoxy)-N-(1-phenylethyl)acetamide derivatives. The compounds containing 1-phenylethylamine as basic moiety attached to substituted phenols were assessed for their anticancer activity against MCF-7 (breast cancer), SK-N-SH (neuroblastoma), anti-inflammatory activity, and analgesic activity. These investigations revealed that synthesized products3a–jwith halogens on the aromatic ring favors as the anticancer and anti-inflammatory activity. Among all, compound3cN-(1-(4-chlorophenyl)ethyl)-2-(4-nitrophenoxy)acetamide exhibited anticancer, anti-inflammatory, and analgesic activities. In conclusion,3cmay have potential to be developed into a therapeutic agent.
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Bonta, Ramesh K. "Dietary Phenolic Acids and Flavonoids as Potential Anti-Cancer Agents: Current State of the Art and Future Perspectives." Anti-Cancer Agents in Medicinal Chemistry 20, no. 1 (2020): 29–48. http://dx.doi.org/10.2174/1871520619666191019112712.
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Background: Cancer is a rapidly growing disease and the second most leading cause of death worldwide. Breast, colon, lung, and prostate cancer are the most diagnosed types of cancer among the majority of the population. The prevalence of these cancers is increasing rapidly due to the lack of effective drugs. The search for anti-cancer bioactive components from natural plant sources is gaining immense significance. The aim of the paper is to introduce the readers about the in vitro and in vivo biochemical mechanisms of phenolic acids and flavonoids in these four types of cancers. Methods: A literature search was carried out in databases, including Scopus, SciFinder, Springer, Science direct and Google. The main keywords used were fruits & vegetables, phenolic acids, flavonoids, anticancer, bioavailability, etc. The data obtained were integrated and analyzed. Results: The study revealed the potential molecular mechanisms of phenolic acids and flavonoids, which include the induction of apoptosis, inhibition of cell proliferation, cell-cycle arrest, induction of Poly ADP ribose polymerase cleavage, downregulation of Matrix metalloproteinases-2 and Matrix metalloproteinases-9 activities, decreased levels of B-cell lymphoma-2, etc. Promising effects of phenolic acids and flavonoids have been observed against breast, colon, lung and prostate cancers. Conclusion: The in vitro and in vivo anti-cancer mechanisms of phenolic acids and flavonoids have been revealed in this study. With the knowledge of specific molecular targets and the structural-functional relationship of bioactive compounds, the current review will open a new gateway for the scientific community and provide them a viable option to exploit more of these compounds for the development of novel and efficacious anticancer compounds.
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Tiwari, Shailee, Nawaz Sharif, Rekha Gajare, et al. "New 2-Oxoindolin Phosphonates as Novel Agents to Treat Cancer: A Green Synthesis and Molecular Modeling." Molecules 23, no. 8 (2018): 1981. http://dx.doi.org/10.3390/molecules23081981.
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The work reports the facile synthesis of novel α-aminophosphonate derivatives coupled with indole-2,3-dione moieties, namely the diethyl(substituted phenyl/heteroaryl)(2-(2-oxoindolin-3-ylidene)hydrazinyl)methylphosphonates derivatives 4(a–n). One-pot three component Kabachnik-Fields reactions were used to synthesize these derivatives. The reaction was carried out at room temperature by stirring in presence of ceric ammonium nitrate (CAN) as a green catalyst. The structures of the synthesized compounds were established by spectral studies. The synthesized derivatives 4(a–n) were evaluated for their in vitro anticancer activity against six human cancer cell lines by the SRB assay method. The cancer cell lines used in this research work are SK-MEL-2 (melanoma), MCF-7 (breast cancer), IMR-32 (neuroblastoma) MG-63 (human osteosarcoma), HT-29 (human colon cancer) and Hep-G2 (human hepatoma). All the synthesized derivatives inhibited the cell proliferation. Importantly, all the target compounds showed no cytotoxicity towards normal tissue cells (GI50 > 250 µM). A docking study was performed to predict the mode of action. Docking results indicate that the compounds have good binding with the enzyme tyrosine kinase as well as with microtubules, which makes them dual inhibitors. The result of in-silico bioavailability studies suggests that the compounds from the present series have good oral drug-like properties and are non-toxic in nature. In vivo acute oral toxicity study results indicate that the compounds can be considered safe, and therefore could be developed in the future as good anticancer agents or as leads for the design and synthesis of novel anticancer agents.
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Haggag, Yusuf, Kyle Matchett, Robert Falconer, et al. "Novel Ran-RCC1 Inhibitory Peptide-Loaded Nanoparticles Have Anti-Cancer Efficacy In Vitro and In Vivo." Cancers 11, no. 2 (2019): 222. http://dx.doi.org/10.3390/cancers11020222.
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The delivery of anticancer agents to their subcellular sites of action is a significant challenge for effective cancer therapy. Peptides, which are integral to several oncogenic pathways, have significant potential to be utilised as cancer therapeutics due to their selectivity, high potency and lack of normal cell toxicity. Novel Ras protein-Regulator of chromosome condensation 1 (Ran-RCC1) inhibitory peptides designed to interact with Ran, a novel therapeutic target in breast cancer, were delivered by entrapment into polyethylene glycol-poly (lactic-co-glycolic acid) PEG-PLGA polymeric nanoparticles (NPs). A modified double emulsion solvent evaporation technique was used to optimise the physicochemical properties of these peptide-loaded biodegradable NPs. The anti-cancer activity of peptide-loaded NPs was studied in vitro using Ran-expressing metastatic breast (MDA-MB-231) and lung cancer (A549) cell lines, and in vivo using Solid Ehrlich Carcinoma-bearing mice. The anti-metastatic activity of peptide-loaded NPs was investigated using migration, invasion and colony formation assays in vitro. A PEG-PLGA-nanoparticle encapsulating N-terminal peptide showed a pronounced antitumor and anti-metastatic action in lung and breast cancer cells in vitro and caused a significant reduction of tumor volume and associated tumor growth inhibition of breast cancer model in vivo. These findings suggest that the novel inhibitory peptides encapsulated into PEGylated PLGA NPs are delivered effectively to interact and deactivate Ran. This novel Ran-targeting peptide construct shows significant potential for therapy of breast cancer and other cancers mediated by Ran overexpression.
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Wang, Li-Ping, Zhi Xu, Gui-Ying Deng, and Sha-Li Xu. "Antiproliferative Activity of 8-methoxy Ciprofloxacin-Hydrozone/Acylhydrazone Scaffolds." Current Topics in Medicinal Chemistry 20, no. 21 (2020): 1911–15. http://dx.doi.org/10.2174/1568026620666200603105644.
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Aims: A series of 8-methoxy ciprofloxacin- hydrazone/acylhydrazone hybrids were evaluated for their activity against a panel of cancer cell lines including HepG2 liver cancer cells, MCF-7, doxorubicin- resistant MCF-7 (MCF-7/DOX) breast cancer cells, DU-145 and multidrug-resistant DU145 (MDR DU-145) prostate cancer cells to seek for novel anticancer agents. Background: Ciprofloxacin with excellent pharmacokinetic properties as well as few side effects, is one of the most common used antibacterial agents. Notably, Ciprofloxacin could induce cancer cells apoptosis, and cell cycle arrest at the S/G2 stage. The structure-activity relationship reveals that the introduction of the methoxy group into the C-8 position of the fluoroquinolone moiety has resulted in a greater binding affinity to the binding site, and 8-methoxy ciprofloxacin derivatives have proved a variety of biological activities even against drug-resistant organisms. However, to the best of our current knowledge, there are no studies that have reported the anticancer activity of 8-methoxy ciprofloxacin derivatives so far. Furthermore, many fluoroquinolone-hydrazone/acylhydrazone hybrids possess promising anticancer activity. Thus, it is rational to screen the anticancer activity of 8-methoxy ciprofloxacin derivatives. Objective: To enrich the structure-activity relationship and provide new anticancer candidates for further investigations. Methods: The desired 8-methoxy ciprofloxacin-hydrazone/acylhydrazone hybrids 5 and 6 were screened for their in vitro anticancer activity against liver cancer cells HepG2, breast cancer cells MCF-7, MCF7/DOX, prostate cancer cells DU-145 and MDR DU-145 by MTT assay. Results: Some of 8-methoxy ciprofloxacin-hydrazone hybrids showed potential activity against HepG2, MCF-7, MCF-7/DOX, DU-145 and MDR DU-145 cancer cell lines, low cytotoxicity towards VERO cells and promising inhibitory activity on tubulin polymerization. Conclusion: Compounds 5d and 5f showed promising anticancer activity, low cytotoxicity, and potential tubulin polymerization inhibitory activity, were worthy of investigation. Other: The structure-activity relationship was enriched.
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Ogloblina, Anna M., Nunzia Iaccarino, Domenica Capasso, et al. "Toward G-Quadruplex-Based Anticancer Agents: Biophysical and Biological Studies of Novel AS1411 Derivatives." International Journal of Molecular Sciences 21, no. 20 (2020): 7781. http://dx.doi.org/10.3390/ijms21207781.
Full textAbstract:
Certain G-quadruplex forming guanine-rich oligonucleotides (GROs), including AS1411, are endowed with cancer-selective antiproliferative activity. They are known to bind to nucleolin protein, resulting in the inhibition of nucleolin-mediated phenomena. However, multiple nucleolin-independent biological effects of GROs have also been reported, allowing them to be considered promising candidates for multi-targeted cancer therapy. Herein, with the aim of optimizing AS1411 structural features to find GROs with improved anticancer properties, we have studied a small library of AS1411 derivatives differing in the sequence length and base composition. The AS1411 derivatives were characterized by using circular dichroism and nuclear magnetic resonance spectroscopies and then investigated for their enzymatic resistance in serum and nuclear extract, as well as for their ability to bind nucleolin, inhibit topoisomerase I, and affect the viability of MCF-7 human breast adenocarcinoma cells. All derivatives showed higher thermal stability and inhibitory effect against topoisomerase I than AS1411. In addition, most of them showed an improved antiproliferative activity on MCF-7 cells compared to AS1411 despite a weaker binding to nucleolin. Our results support the hypothesis that the antiproliferative properties of GROs are due to multi-targeted effects.
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Kharb, Manju, Pawan Jalwal, Shikha Rathi, and Suresh Kumar. "Preparation and Characterization of Novel Anti-cancer drug (s) loaded Co-crystals." Journal of University of Shanghai for Science and Technology 23, no. 09 (2021): 1006–19. http://dx.doi.org/10.51201/jusst/21/09647.
Full textAbstract:
Background: Taxanes constitute an important class of anti-cancer agents, which are widely prescribed for the management of cancers like breast, lung and ovaries. These agents belong to Biopharmaceutical Classification System (BCS) class IV, which are neither soluble in the aqueous systems nor permeable across the biological membranes. Objectve: Due to these concerns only, the oral bioavailabilities of these drugs are too low. Looking into these concerns, it was envisaged to develop co-crystals of docetaxel with syringic acid. Methods: For the preparation of co-crystals no single method is used. The methods range from spray drying, crystallization, ultrasonication and freeze drying to supercritical fluid methodologies. Results: The novel co-crystal not only improved the solubility and dissolution rates of the drug, but also resulted in improved pharmacokinetic profile. Conclusion: The present findings provide an economic and viable approach to improve the solubility and absorption profile of a drug, which is a vital component of the anticancer chemotherapy. Such studies provide a hope for the development of approaches to improve the solubility and permeability of drugs with challenges.
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Wu, Tong, Ting Li, Ya-Nan Kang, et al. "Synthesis and Biological Evaluation of Novel Alkyl Amine Substituted Icariside II Derivatives as Potential Anticancer Agents." Molecules 23, no. 9 (2018): 2146. http://dx.doi.org/10.3390/molecules23092146.
Full textAbstract:
A series of novel alkyl amine-substituted icariside II (ICA II) derivatives were synthesized by Mannich reactions at the 6-C position (compounds 4a–d) and changing the carbon chain length at the 7-OH position (compounds 7a–h), and their in vitro antitumor activity towards human breast cancer lines (MCF-7 and MDA-MB-231) and human hepatoma cell lines (HepG2 and HCCLM3-LUC) were evaluated by the MTT assay. Compared with ICA II, most of the twelve derivatives showed good micromole level activity and a preliminary structure-activity relationship (SAR) for the anticancer activity was obtained. Compound 7g showed the most potent inhibitory activity for the four cancer cell lines (13.28 μM for HCCLM3-LUC, 3.96 μM for HepG2, 2.44 μM for MCF-7 and 4.21 μM for MDA-MB-231), which was 2.94, 5.54, 12.56 and 7.72-fold stronger than that of ICA II. The preliminary SAR showed that the introduction of a alkyl amine substituent at 6-C was not favorable for the anticancer activity, while most of the 7-O-alkylamino derivatives exhibited good antitumor activity and the anticancer activity 7-O-alkylamino derivatives were influenced by the alkyl chain length and the different terminal amine substituents. Furthermore, the effects of compound 7g on apoptosis and cell cycle of MCF-7 cells were further investigated, which showed that compound 7g triggered apoptosis and arrested the cell cycle at the G0/G1 phase in MCF-7 cells. Our findings indicate that compound 7g may be a promising anticancer drug candidate lead.
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Amr, Abd, Elsayed Elsayed, Mohamed Al-Omar, Hanan Badr Eldin, Eman Nossier, and Mohamed Abdallah. "Design, Synthesis, Anticancer Evaluation and Molecular Modeling of Novel Estrogen Derivatives." Molecules 24, no. 3 (2019): 416. http://dx.doi.org/10.3390/molecules24030416.
Full textAbstract:
A series of estrone derivatives 3–8 was designed and synthesized using estrone arylmethylenes 2a,b as starting materials and their structures were confirmed by different spectral data and elemental analyses. All the newly synthesized compounds exhibited potent in vitro and in vivo cytotoxic activities against breast cancer cell lines. In addition, all compounds were subjected to in vitro and in vivo inhibition assays for EGFR and VEGFR-2 kinases as well as p53 ubiquitination activity to obtain more details about their mechanism of action. Based on the promising results, a molecular docking study was investigated for the most representative compound 5a against the two targets, EGFR and VEGFR-2 kinases, to assess its binding affinity, hoping to rationalize and obtain potent anticancer agents in the future.
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Rahman, Faiz-Ur, Amjad Ali, Rong Guo, et al. "Synthesis and anticancer activities of a novel class of mono- and di-metallic Pt(ii)(salicylaldiminato)(DMSO or Picolino)Cl complexes." Dalton Transactions 44, no. 5 (2015): 2166–75. http://dx.doi.org/10.1039/c4dt03018d.
Full textAbstract:
Mono- and di-metallic Pt(ii)(salicylaldiminato)(DMSO or Picolino)Cl complexes as potential cytotoxic agents against tested human breast (MCF-7), liver (HepG2), lung (A549), colon (HCT116) and cervical (Hela) cancer cell lines.
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Day, Candace M., Shane M. Hickey, Yunmei Song, Sally E. Plush, and Sanjay Garg. "Novel Tamoxifen Nanoformulations for Improving Breast Cancer Treatment: Old Wine in New Bottles." Molecules 25, no. 5 (2020): 1182. http://dx.doi.org/10.3390/molecules25051182.
Full textAbstract:
Breast cancer (BC) is one of the leading causes of death from cancer in women; second only to lung cancer. Tamoxifen (TAM) is a hydrophobic anticancer agent and a selective estrogen modulator (SERM), approved by the FDA for hormone therapy of BC. Despite having striking efficacy in BC therapy, concerns regarding the dose-dependent carcinogenicity of TAM still persist, restricting its therapeutic applications. Nanotechnology has emerged as one of the most important strategies to solve the issue of TAM toxicity, owing to the ability of nano-enabled-formulations to deliver smaller concentrations of TAM to cancer cells, over a longer period of time. Various TAM-containing-nanosystems have been successfully fabricated to selectively deliver TAM to specific molecular targets found on tumour membranes, reducing unwanted toxic effects. This review begins with an outline of breast cancer, the current treatment options and a history of how TAM has been used as a combatant of BC. A detailed discussion of various nanoformulation strategies used to deliver lower doses of TAM selectively to breast tumours will then follow. Finally, a commentary on future perspectives of TAM being employed as a targeting vector, to guide the delivery of other therapeutic and diagnostic agents selectively to breast tumours will be presented.
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KSNM, Megana, and Suneetha Y. "VIRTUAL SCREENING AND IDENTIFICATION OF PLAUSIBLE NOVEL THERAPEUTIC EGFR INHIBITORS AGAINST BREAST CANCER." Journal of Experimental Biology and Agricultural Sciences 9, no. 4 (2021): 481–91. http://dx.doi.org/10.18006/2021.9(4).481.491.
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Present days increasing concern about the identification of potential non-toxic drug candidates against several cancers is very important. The current study was carried out to discover the novel phytochemicals as effective anticancer agents against the selected protein (i.e., EGFR), which is a promising target for moderating triple-negative breast cancer (TNBC). Various studies showed that the natural constituents have a strong anti-tumor capacity and inhibiting tumor growth. Here structure-based virtual screening and molecular docking studies have been recognized as rational tactics for the recognition of novel drug candidates against the binding domain of EGFR (PDB code: 3GKW & 5FEE). Furthermore, the drug-likeness, adverse effects, and toxicogenomics effects were assessed with the help of various computational tools. Virtual screening was reported that 4 drug candidates i.e., CID: 65064; CID: 5280443; CID: 440735, and CID: 5280343 showed reliable consequences with fewer side effects and more efficient for the selected proteins. The overall effects indicated that renowned hits could be developed as reference skeletons for novel inhibitors envisaging EGFR to ameliorate TNBC.
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Pugachev, Mikhail V., Thang T. N. Nguyen, Timur M. Bulatov, et al. "Synthesis and Antitumor Activity of Novel Pyridoxine-Based Bioisosteric Analogs of trans-Stilbenes." Journal of Chemistry 2017 (2017): 1–7. http://dx.doi.org/10.1155/2017/8281518.
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A series of trans-6-phenylethenyl substituted pyridoxine derivatives, novel bioisosteric analogs of drugs based on trans-stilbene scaffold, were synthesized using the Wittig reaction of a bis-triphenylphosphonium pyridoxine derivative with various aromatic aldehydes. Two compounds demonstrated high activity against the estrogen-dependent MCF-7 (breast cancer) cell line with IC50 in the range of 1.9–7.9 µM and very good selectivity for other studied normal and tumor cells, including the estrogen receptor negative MDA-MB-231 breast cancer cells. The active compounds possessed an intense blue fluorescence, and this feature allowed us to effectively visualize them in cytoplasm and in nucleus. The obtained results make the described chemotype a promising starting point for the development of new anticancer agents for the therapy of estrogen-dependent malignancies.
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Eid, Ahmad M., Mohammed Hawash, Johnny Amer, et al. "Synthesis and Biological Evaluation of Novel Isoxazole-Amide Analogues as Anticancer and Antioxidant Agents." BioMed Research International 2021 (March 9, 2021): 1–9. http://dx.doi.org/10.1155/2021/6633297.
Full textAbstract:
Cancer now is one of the leading causes of mortality in the world. There has been a lot of effort to discover new anticarcinogenic agents that allow treatment with fewer side effects. A series of isoxazole-carboxamide derivatives (2a–2g) were synthesised and evaluated for their cytotoxic activity against breast (MCF-7), cervical (HeLa), and liver (Hep3B) cancer cell lines and their antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The results showed that 2d and 2e were the most active compounds against Hep3B cells, with a half-maximal inhibitory concentration (IC50) of around 23 μg/ml; 2d showed the highest activity against HeLa cells, with an IC50 15.48 μg/ml. However, 2a had the lowest IC50 (39.80 μg/ml) against MCF-7 cells. By contrast, compound 2g was inactive against all cancer cell lines, with IC50 values >400 μg/ml. Both 2d and 2e reduced Hep3B secretion of alpha-fetoprotein (to 1829.33 ± 65.91 ng / ml and 1758.66 ± 54.04 ng / ml , respectively). Furthermore, in cell cycle analysis, 2d and 2e induced a delay in the G2/M phase of 18.07%, which is similar to the doxorubicin positive control. Moreover, 2d and 2e reduced the necrosis rate of Hep3B threefold and instead shifted the cells to apoptosis. Our results indicate that 2d and 2e have potent and promising anticancer activity. However, compound 2a was the most active as antioxidant agent ( I C 50 = 7.8 ± 1.21 μ g / ml ) compared with Trolox as a positive control (IC50 2.75 μg/ml).