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Journal articles on the topic 'Anticancer compound'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Yaprak, Yıldız, HülyaAkgün, Sipahi Hande, Deniz İnci, and Berk Barkın. "Synthesis, Characterization and Potential Anticancer and Antimicrobial Activities of New Phthalamide Derivatives." Pharmaceutical and Chemical Journal 6, no. 1 (2019): 72–83. https://doi.org/10.5281/zenodo.13931678.

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A series of N<sup>1</sup>,N<sup>2</sup>-bis [(2-substitutedphenyl)ethyl]phthalamide (compounds <strong>1-10</strong>) and 3-nitro-N<sup>1</sup>, N<sup>2</sup>-bis [(2-substitutedphenyl)ethyl]phthalamide (compounds <strong>11-20</strong>) were synthesized. Their structures and purity were analyzed by IR, <sup>1</sup>H-NMR spectra and elemental analysis. The compounds were evaluated for their <em>in vitro </em>cytotoxicity against the MCF7 and Hep3B cancer cell lines. Cytotoxicity screening revealed that N<sup>1</sup>,N<sup>2</sup>-bis[2-(2,4-dichlorophenyl)ethyl]phthalamide (compound<strong> 5<

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2

Firdaus, Firdaus, Nunuk Hariani Soekamto, Seniwati Seniwati, et al. "Phenethyl p-coumarate and N-phenethyl-p-coumaramide: Synthesis, Characterization, Docking Studies, and Anticancer Activity through P388 Cell." Sains Malaysiana 51, no. 4 (2022): 1085–97. http://dx.doi.org/10.17576/jsm-2022-5104-11.

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Most p-coumaric acid derivatives and molecules containing phenethyl moiety have a potential in anticancer activity. Thus, combining a p-coumaroyl group and a phenethyl moiety in one compound will increase anticancer activity. The principal objective of this research was to incorporate p-coumaroyl and phenethyl moieties to form an ester, phenethyl p-coumarate (5), and an amide, N-phenethyl-p-coumaramide (6), then tested their anticancer activity using P388 leukemia murine cells. The characterization by FTIR method, compound 5 gave a strong absorption band of alkyl C-O bond that appears at 1165,

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3

Haggam, Reda Ahmed, Mohamed Gomma Assy, Mohamed Hassan Sherif, and Mohamed Mohamed Galahom. "A series of 1,3-imidazoles and triazole-3-thiones based thiophene-2-carboxamides as anticancer agents: Synthesis and anticancer activity." European Journal of Chemistry 9, no. 2 (2018): 99–106. http://dx.doi.org/10.5155/eurjchem.9.2.99-106.1701.

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By addition of semicarbazide or phenylhydrazine hydrochloride to thienoylisothiocyanate (1) resulted in building of thiosemicarbazide derivative (2), triazole derivative (4) and thiophene-2-carboxamide (5), respectively. Basic cyclization of compound 2 led to formation of oxadiazine (3). Synthesis of thiadiazine derivative (6) was achieved via reaction of compound 5 and maleic anhydride in triethyl amine. Heating of compound 5 with ethyl chloroacetate or sodium ethoxide produced thiadiazine derivative (7) and triazolethione (8), respectively. Thiosemicarbazide derivative 11 was synthesized by

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4

Sonawane, Ganesh, Shweta Sharma, and Ritu Gilhotra. "Synthesis, Characterization and Pharmacological Screening of 1,3,4-Oxadiazoles." Asian Journal of Chemistry 36, no. 6 (2024): 1436–46. http://dx.doi.org/10.14233/ajchem.2024.31776.

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Two series of 1,3,4-oxadiazole scaffolds (10a-j & 12a-j) were synthesized and comprehensively characterized using IR, NMR and mass spectra. Subsequently, the synthesized compounds underwent screening for anticancer activity against HepG2 and MCF-7 cell lines. All the 20 compounds exhibited substantial anticancer activity with compounds 10b and 10e demonstrating particularly significant activity surpassing that of the standard 5-fluorouracil. Significantly, compound 10b displayed superior efficacy compared to compound 10e, prompting its selection for further in vivo assessment against dieth

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5

Thiriveedhi, Arunkumar, Ratnakaram Venkata Nadh, Navuluri Srinivasu, and Narayana Murthy Ganta. "Novel Pyrazolyl Benzoxazole Conjugates: Design, Synthesis, Molecular Docking Studies and in vitro Anticancer Activities." Letters in Organic Chemistry 16, no. 8 (2019): 619–26. http://dx.doi.org/10.2174/1570178615666181022141919.

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Nowadays, hybrid drugs have gained a significant role in the treatment of different health problems. Most of the hybrid molecules with different heterocyclic moieties were proved to be potent anti-tumor agents in cancer chemotherapy. Hence, the present study is aimed at the evaluation of in vitro anticancer activity of novel hybrid molecules (pyrazolyl benzoxazole conjugates) and to investigate their anticancer activity by molecular docking studies. Designed, synthesized and characterized the novel pyrazolyl benzoxazole conjugates. Anticancer activity of these compounds was determined by SRB a

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6

Akrami, Hamidreza, Bibi Fatemeh Mirjalili, Omidreza Firuzi, et al. "Cytotoxic Activity and DNA Binding Property of New Aminopyrimidine Derivatives." Letters in Drug Design & Discovery 17, no. 5 (2020): 640–54. http://dx.doi.org/10.2174/1570180816666190712102119.

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Background: Chromene and anilinopyrimidine heterocyclics are attractive anticancer compounds that have inspired many researchers to design novel derivatives bearing improved anticancer activity. Methods: A series of pyrimidine-fused benzo[f]chromene derivatives 6a-x were synthesized as anticancer hybrids of 1H-benzo[f]chromenes and anilinopyrimidines. The inhibitory activity of the synthesized compounds 6a-x against cell viability of human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (MOLT-4) and human breast adenocarcinoma (MCF-7) cell lines was evaluated using MTT

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7

Honavar, Premanand M., Bhuvanesh Sukhlal Kalal, Ranjith Raj, et al. "Thiazolyl-Thiazolidinone Conjugated Pyrazoles as Potential Anticancer and Antibacterial Agents and Molecular Docking Studies." Asian Journal of Chemistry 36, no. 12 (2024): 2855–60. https://doi.org/10.14233/ajchem.2024.32708.

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In current study, five new compounds containing thiazolyl-thiazolidinone conjugated substituted pyrazoles were prepared and screened for anticancer and antimicrobial activities. Synthesized compounds were characterized by spectroscopic techniques. Anticancer activity was carried out against human melanoma cancer A375 and human breast cancer MDA-MB-231 cell lines. Also, these were screened for antibacterial activity against two Gram-positive Staphylococcus aureus, Bacillus subtilis strains and three Gram-negative Pseudomonas aeruginosa, Klebsiella pneumonia and Escherichia coli strains. Antican

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8

Omar, Ashraf M., Heba A. Abd El Razik, Aly A. Hazzaa, et al. "New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential." Future Medicinal Chemistry 11, no. 13 (2019): 1583–603. http://dx.doi.org/10.4155/fmc-2018-0285.

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Aim: Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. Materials & methods: Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. Results: Compound 7 showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound 6f displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds 5b, 6a, 6c, 6d and 8 were found to be more active antioxidants than trolox. Compounds 6a, 6c, 6f and 8 revealed high COX-2 inhibito

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9

Guan, Yong-Feng, Xiu-Juan Liu, Xin-Ying Yuan, et al. "Design, Synthesis, and Anticancer Activity Studies of Novel Quinoline-Chalcone Derivatives." Molecules 26, no. 16 (2021): 4899. http://dx.doi.org/10.3390/molecules26164899.

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The chalcone and quinoline scaffolds are frequently utilized to design novel anticancer agents. As the continuation of our work on effective anticancer agents, we assumed that linking chalcone fragment to the quinoline scaffold through the principle of molecular hybridization strategy could produce novel compounds with potential anticancer activity. Therefore, quinoline-chalcone derivatives were designed and synthesized, and we explored their antiproliferative activity against MGC-803, HCT-116, and MCF-7 cells. Among these compounds, compound 12e exhibited a most excellent inhibitory potency a

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10

Huang, Jiuhong, Juanli Wang, Guiting Song, et al. "Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell." Molecules 27, no. 24 (2022): 8844. http://dx.doi.org/10.3390/molecules27248844.

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Colorectal cancer (CRC) is one of the most common causes of cancer-related death worldwide, and more therapies are needed to treat CRC. To discover novel CRC chemotherapeutic molecules, we used a series of previously synthesized novel imidazolidin-4-one derivatives to study their anticancer role in several cancer cell lines. Among these compounds, compound 9r exhibited the best anticancer activity in CRC cell lines HCT116 and SW620. We further investigated the anticancer molecular mechanism of compound 9r. We found that compound 9r induced mitochondrial pathway apoptosis in HCT116 and SW620 ce

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11

Asman, Sadino, Permana Benny, Suherman Meilia, and Noviartika Fuji Ayu. "3D-PHARMACOPHORE MODELING AND MOLECULAR DOCKING TO STUDY THE POTENTIAL ANTI-CANCER AGENT FROM Ficus septica Burm. L." Pharmacoscript 5, no. 1 (2022): 24–37. http://dx.doi.org/10.36423/pharmacoscript.v5i1.756.

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In vitro testing showed that awar awar (Ficus septica Burm. L ) leaf had an anticancer activity. Ethanol extract from awar-awar leaves could selectively inhibit cancer cell growth with IC50 values, there were MCF7 breast cancer cells (48 µg/ml), HeLa cervical cancer cells (122.4 µg/mL), and WiDR cancer cells (75.9 µg/mL). However, the active compounds that play a role in inhibiting the three cancer cells are not yet found. Therefore, this research carried out to find out the active compound using in silico. 3D-pharmacophore modeling and Molecular docking were developed for finding out the pote

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12

Gaber, Ahmed, Walaa F. Alsanie, Majid Alhomrani, Abdulhakeem S. Alamri, Ibrahim M. El-Deen, and Moamen S. Refat. "Synthesis of 1-[(Aryl)(3-amino-5-oxopyrazolidin-4-ylidene) methyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic Acid Derivatives and Their Breast Anticancer Activity." Crystals 11, no. 5 (2021): 571. http://dx.doi.org/10.3390/cryst11050571.

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This research aimed to produce new 1-[(aryl)(3-amino-5-oxopyrazolidin-4-ylidene) methyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic acid derivatives and check their anticancer effect against the breast cancer MCF-7 cell line. The 2-oxo-1,2-dihydroquinoline-3-carboxylic acid (4) compound was obtained by hydrolyzing ethyl 2-oxo-1,2-dihydroquinoline-3-carboxylate (2) with thiourea and anhydrous potassium carbonate ethanol, which was then treated with ethyl 3-substituted 2-cyanoacrylates (6) in the presence of triethylamine in diethyl formamide to give 1-[2-(ethoxy)carbonyl-2-cyano-1-arylvinyl]-2-oxo

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13

BAŞARAN, Eyüp, Reşit ÇAKMAK, Ercan ÇINAR, and Ozge CEVİK. "Some Heterocyclic Hydrazone Compounds: Synthesis, Spectral Characterization and Anticancer Activity Study." Cumhuriyet Science Journal 43, no. 3 (2022): 437–42. http://dx.doi.org/10.17776/csj.1099217.

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Cancer is currently ongoing to be a significant health problem threatening human health. Hydrazone compounds constitute a popular class of organic compounds used in novel drug discovery studies in therapy of cancer. In the current study, the preparation and structural characterization of some heterocyclic hydrazone compounds (7-12) and their anticancer capacities against HeLa cervical cancer and MCF-7 breast cancer cell lines were reported. The target compounds were characterized by some spectroscopic techniques (1H NMR, 13C NMR and FT-IR). The in vitro cytotoxic potentials of the target molec

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14

Husain, Asif, Silky Bedi, Shazia Parveen, et al. "Furanone-functionalized benzothiazole derivatives: synthesis, in vitro cytotoxicity, ADME, and molecular docking studies." Zeitschrift für Naturforschung B 77, no. 1 (2021): 41–53. http://dx.doi.org/10.1515/znb-2021-0146.

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Abstract In the present study, a novel series of new furanone-based benzothiazole derivatives (4a-j) were synthesized from 4-(benzo[d]thiazol-2-yl)-4-oxobutanoic acid (3) as potential anticancer agents. In vitro cytotoxicity against three human cancer cell lines (A549, MCF7, and DUI45) revealed substantial activity. Di-substituted compound, 4i emerged as a promising anticancer compound which showed IC50 values of 7.2 ± 0.5, 6.6 ± 1.4, and 7.3 ± 0.1 µM against A549, MCF7, and DUI45 cell lines, respectively. Four compounds 4c, 4e, 4f, and 4i evaluated for their acute toxicity were found to be no

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15

Devi, Brindha, Rajagopala K, and Esther Elizabeth. "PHARMACOPHORIC SCREENING OF VARIOUS ENDOPHYTIC FUNGAL METABOLITES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 5 (2017): 140. http://dx.doi.org/10.22159/ajpcr.2017.v10i5.17157.

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Objective: To screen various endophytic fungal metabolites toward anti-inflammatory, anticancer, and antioxidant property virtually.Methods: In this study, 14 bioactive compounds reported from endophytic fungi have taken for structure-based drug design. With the help of softwareSchrodinger, different modules were used to perform screening of top active compounds. Ligprep, epharm, Glide, Quikprop are the modules were used from the software for our study. Identification of leads, pharmacophore model generation, and molecular docking studies were assessed using this software.Results: After the sc

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16

Desai, S. N. Mamle, Rudrax N. S. Priolkar, Harshank A. Naik Karmali, Prabhav D. Ambe, and B. S. Biradar. "SYNTHESIS, CHARACTERIZATION AND EVALUATION OF 4-HYDROXY-1-PHENYL/METHYL-3-(3-SUBSTITUTED-1-(SUBSTITUTEDIMINO) PROPYL) QUINOLINE-2(1H)-ONE DERIVATIVES AND 4-HYDROXY-1-PHENYL/METHYL-3-(1-(SUBSTITUEDIMINO) ETHYL) QUINOLINE-2(1H)-ONE DERIVATIVES AS POSSIBLE ANTICANCER AGENTS." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 10 (2017): 240. http://dx.doi.org/10.22159/ijpps.2017v9i10.20184.

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Objective: Synthesis, characterization and evaluation of quinolin-2-one derivatives as possible anticancer agents.Methods: A series of novel 4-hydroxy-1-phenyl/methyl-3-(3-substituted-1-(substitutedimino)propyl)quinolin-2(1H)-one derivatives IIa(1-5)/IIb(1-5) and 4-hydroxy-1-phenyl/methyl-3-(1-(substituedimino)ethyl)quinolin-2(1H)-one derivatives IIIa(1-3)/IIIb(1-3) were synthesised by nucleophilic addition of substituted anilines on 3-acetyl-4-hydroxy-1-phenyl/methylquinolin-2(1H)-one (a/b) and 4-hydroxy-3-(3-substitutedpropanoyl)-1-phenyl/methyl quinolin-2(1H)-one (Ia/Ib); respectively. The

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17

Zhou, Yuanyuan, Zhongguo Zhou, Dessy Chan, et al. "The Anticancer Effect of a Novel Quinoline Derivative 91b1 through Downregulation of Lumican." International Journal of Molecular Sciences 23, no. 21 (2022): 13181. http://dx.doi.org/10.3390/ijms232113181.

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Quinoline derivatives have been reported to possess a wide range of pharmaceutical activities. Our group previously synthesized a series of quinoline compounds, in which compound 91b1 showed a significant anticancer effect. The purpose of this study was to evaluate the anticancer activity of compound 91b1 in vitro and in vivo, and screen out its regulated target. A series of cancer cell lines and nontumor cell lines were treated with compound 91b1 by MTS cytotoxicity assay and cell-cycle assay. In vivo anticancer activity was evaluated by a xenografted model on nude mice. Target prediction of

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18

Alanazi, Mohammed M., and Ashwag S. Alanazi. "Novel 7-Deazapurine Incorporating Isatin Hybrid Compounds as Protein Kinase Inhibitors: Design, Synthesis, In Silico Studies, and Antiproliferative Evaluation." Molecules 28, no. 15 (2023): 5869. http://dx.doi.org/10.3390/molecules28155869.

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Cancer is a multifactorial disorder with extremely complex genetics and progression. The major challenge in cancer therapy is the development of cancer resistance and relapse. Conventional anticancer drugs directly target the DNA of the cell, while modern chemotherapeutic drugs include molecular-targeted therapy, such as targeting the abnormal cell signaling inside the cancer cells. Targeted chemotherapy is effective in several malignancies; however, the success has always been limited by drug resistance and/or side effects. Anticancer with multi-targeted actions simultaneously modulates multi

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19

Patel, Rajat, Puja Sharma, Rohit R. Koshti, Akshay Vyas, and Chetan B. Sangani. "Synthesis, Characterization and Molecular Modeling of Pyrazole-Quinoline Hybrids as New Class of Antibacterial, Antimicrobial, Anticancer Agents and DFT Study." Asian Journal of Chemistry 35, no. 4 (2023): 828–38. http://dx.doi.org/10.14233/ajchem.2023.26894.

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A new series of pyrazole-quinoline hybrids were synthesized by a base-catalyzed cyclocondensation reaction through one-pot multi-component reaction, based on molecular hybridization techniques. All the compounds 10a-x were examined for in vitro antibacterial and anticancer activities. Enzyme inhibitory activities were carried out against FabH and EGFR. From the studied compounds, most of the compounds showed effective antibacterial as well as anticancer activity against used strains and cancer cell lines, respectively. The most potent inhibitory activity was displayed by compound 10r against E

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20

Sanuddin, Mukhlis, Indri Meirista, and Siska Emilia Nasril. "TESTING THE ACTIVITY OF THE SYNTHETIC COMPOUND DIPHENYLTIN (IV)N- BENZYL METHYL DITHIOCARBAMATE AGAINST BREAST CANCER MCF-7." International Journal of Pharmaceutical Sciences and Medicine 7, no. 12 (2022): 97–106. http://dx.doi.org/10.47760/ijpsm.2022.v07i12.006.

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Breast cancer is the leading cause of death, especially for women in Indonesia. Compounds that are widely used for anticancer at present are organotin compounds, one of which is dithiocarbamate compounds, with several reports of antifungal, antibacterial, anticancer, anti-alkylation, and apoptosis-inducing activities of metal dithiocarbamate complexes and their mixed ligands. The purpose of this study was to determine the activity test of the synthetic compound Diphenyltin (IV) N-Benzylmethyldithiocarbamate Against Breast Cancer MCF-7 using the MTT Assay (Microculture Tetrazolium Technique) As

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21

Ezhilarasi, M. R., and Manju Mathew. "Design Synthesis and Spectral Characterization of Novel Morpholine ring fused with Substituted Pyrazoline Derivatives as Promising Anticancer, Antimicrobial Activity of in vitro and in silico studies." Research Journal of Chemistry and Environment 28, no. 8 (2024): 6–15. http://dx.doi.org/10.25303/288rjce06015.

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A search for new anticancer agents has prompted the design and synthesis of new novel morpholine ring fused with substituted pyrazoline derivatives MCP 1-4 as potent anticancer agents. MCP compounds were synthesized and the compounds structures were elucidated using elemental analysis and spectroscopic techniques like FT-IR, 1H NMR and 13C NMR. MCP derivatives binding affinities values were predicted by Auto Dock version, which shows the MCP derivatives as good anticancer 1OQA protein and antimicrobial properties, bacterial protein 1UAG and 5KEE with good binding affinity values from -6.2 to -

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22

Lai, Weihong, Jiaxin Chen, Xinjiao Gao, Xiaobao Jin, Gong Chen, and Lianbao Ye. "Design and Synthesis of Novel Chalcone Derivatives: Anti-Breast Cancer Activity Evaluation and Docking Study." International Journal of Molecular Sciences 24, no. 21 (2023): 15549. http://dx.doi.org/10.3390/ijms242115549.

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Chalcone is a common simple fragment of natural products with anticancer activity. In a previous study, the research group discovered a series of chalcone derivatives with stronger anticancer activities. To find better anticancer drugs, novel chalcone derivatives A1–A14, B1–B14 have continuously been designed and synthesized. The antiproliferative activity of these compounds against breast cancer cells (MCF-7) was investigated by the Cell Counting Kit-8 (CCK-8) method with 5-fluorouracil (5-Fu) as the control drug. The results showed that compound A14 exhibited excellent antiproliferative abil

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23

Yang, Wenzhi, Guangjie Liang, Yang Sun, and Zhijin Gong. "Bioactive Secondary Metabolites from Marine Streptomyces griseorubens f8: Isolation, Identification and Biological Activity Assay." Journal of Marine Science and Engineering 9, no. 9 (2021): 978. http://dx.doi.org/10.3390/jmse9090978.

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Marine actinomycetes are a potential source of a wide variety of bioactive natural products. Herein, four cyclic dipeptides, namely, cyclo(L-Val-L-Pro) (compound 1), cyclo(L-Pro-L-Leu) (compound 2), cyclo(L-Pro-L-Tyr) (compound 3) and cyclo(L-Pro-L-Phe) (compound 5), and an N-acetyltyramine (compound 4) were first isolated and identified as products of the marine Streptomyces griseorubens f8. Compounds 3 and 5 exhibit antibacterial activity against Staphylococcus aureus, Klebsiella aerogenes and Proteus vulgaris. The minimum inhibitory concentrations (MICs) against Staphylococcus aureus, Klebs

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24

Dasari, Raghu, Srinivas Gali, and Namrata Vaddiraju. "Novel carboxamide and carbohydrazide functionalized pyridopyrimidine derivatives and their anticancer activity." Research Journal of Chemistry and Environment 27, no. 5 (2023): 83–90. http://dx.doi.org/10.25303/2705rjce083090.

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A series of novel carboxamide and carbohydrazide functionalized pyridopyrimidine derivatives was prepared starting from 6-methyl/ethyl-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile 1. Compound 1 on reaction with sulphuric acid gave compound 2. Compound 2 on reaction with chloroacetamide followed by reaction with EMME coupling and further cyclization gave compound 5. Compound 5 on reaction with hydrazine hydrate produced hydrazide derivatives 6. Compound 6 on reaction with diverse substituted aromatic aldehyde gave Schiff’s base derivatives 7a-j. Ester derivatives 5 on reaction w

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Sinha, Manish, Baljeet Kaur, Amandeep Kaur, Shruti Kuletha, Karanveer Singh, and Rohit Bhatia. "Anticancer Activity of Aminoacid Linked Novel 4-Methylumbelliferone Derivatives." Current Bioactive Compounds 15, no. 1 (2019): 51–62. http://dx.doi.org/10.2174/1573407213666170210143503.

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Background: Cancer is a disease of high mortality. The therapeutic agents currently available are insufficient to cure it and are associated with serious side effects. 4-methylumbelliferone is a natural product containing benzo-&#945;-pyrones as a central nucleus. Benzo-&amp;#945;-pyrone is a privileged moiety having multifarious biological activities including anticancer activity. A series of compounds were synthesized taking 4-methylumbelliferone as a core nucleus and screened for their anticancer activity against HeLa cancer cell line. Methods: The 4-methylumbelliferone was linked w

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Mostafa, Amany S., Waleed A. Bayoumi, Mohamed El-Mesery, and Abdelaziz Elgaml. "Molecular Design and Synthesis of New 3,4-Dihydropyrimidin-2(1H)-Ones as Potential Anticancer Agents with VEGFR-2 Inhibiting Activity." Anti-Cancer Agents in Medicinal Chemistry 19, no. 3 (2019): 310–22. http://dx.doi.org/10.2174/1871520618666180717125906.

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Background: Two series of 3,4-dihydropyrimidin-2(1H)-one derivatives were designed based on the main structural features characterizing reported anticancer compounds with potent VEGFR-2 inhibiting activity. Methods: All the target compounds were synthesized and investigated for their in vitro anticancer activity using MTT assay and NCI protocol. The most active compounds were further investigated for the VEGFR-2 inhibiting activity using enzyme inhibition assay. Results: Of these derivatives, compound 8b possessed significant activity against Caco-2 (IC50 of 24.9 µM) and MCF7 (IC50 of 29.4 µM)

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Hawash, Mohammed, Ahmad M. Eid, Nidal Jaradat, et al. "Synthesis and Biological Evaluation of Benzodioxole Derivatives as Potential Anticancer and Antioxidant agents." Heterocyclic Communications 26, no. 1 (2020): 157–67. http://dx.doi.org/10.1515/hc-2020-0105.

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Abstracta series of benzodioxole compounds were synthesized and evaluated for their cytotoxic activity against cervical (Hela), colorectal (Caco-2), and liver (Hep3B) cancer cell lines. Compounds 5a, 5b, 6a, 6b, 7a and 7b showed very weak or negligible anticancer activity with IC50 3.94-9.12 mM. On the contrary, carboxamide containing compounds 2a and 2b showed anticancer activity. Both 2a and 2b reduced Hep3B secretions of α-fetoprotein (α-FP) to 1625.8 ng/ml and 2340 ng/ml, respectively, compared to 2519.17 ng/ml in untreated cells. The results also showed that compound 2a has potent antican

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Kornii, Yurii, Oleh Shablykin, Olga Shablykina, and Volodymyr Brovarets. "New 4-iminohydantoin sulfamide derivatives with antiviral and anticancer activity." Ukr. Bioorg. Acta 2021, Vol. 16, N1 16, no. 1 (2021): 10–17. http://dx.doi.org/10.15407/bioorganica2021.01.010.

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A number of sulfamides were obtained by reaction of (5-(dichloromethylene)-2-oxoimidazolidin-4-ylidene)sulfamoyl chloride with anilines, benzylamines, Boc-protected piperazine, methylalylamine, and amino acids methyl esters with primary and secondary amino group. The antiviral and anticancer activity of new derivatives was evaluated. The most effective compounds against Human cytomegalovirus were sulfamides based on anisidine (1b), N-Boc-piperazine (1h), and the derivatives 1n,o with fragments of nipecotic and azetidine-3-carboxylic acids, respectively. Anticancer activity was most significant

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Attia, Adel Mahmoud, Ahmed Ibrahin Khodair, Eman Abdelnasser Gendy, Mohammed Abu El-Magd, and Yaseen Ali Mosa Mohamed Elshaier. "New 2-Oxopyridine/2-Thiopyridine Derivatives Tethered to a Benzotriazole with Cytotoxicity on MCF7 Cell Lines and with Antiviral Activities." Letters in Drug Design & Discovery 17, no. 2 (2020): 124–37. http://dx.doi.org/10.2174/1570180816666190220123547.

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Background:Perturbation of nucleic acids structures and confirmation by small molecules through intercalation binding is an intriguing application in anticancer therapy. The planar aromatic moiety of anticancer agents was inserted between DNA base pairs leading to change in the DNA structure and subsequent functional arrest.Objective:The final scaffold of the target compounds was annulated and linked to a benzotriazole ring. These new pharmacophoric features were examined as antiviral and anticancer agents against MCF7 and their effect on DNA damage was also assessed.Methods:A new series of fu

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30

Abumansour, Hamza, Osama H. Abusara, Mohammad Abu-Sini, et al. "Thionated levofloxacin derivative: Potential repurposing for cancer treatment and synergism with doxorubicin on doxorubicin-resistant lung cancer cells." PLOS One 20, no. 6 (2025): e0324930. https://doi.org/10.1371/journal.pone.0324930.

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Objectives Fluoroquinolones, such as levofloxacin (LVX), are extended-spectrum drugs used for the treatment of bacterial infections. Several fluoroquinolone derivatives have shown promising antibacterial and anticancer activities. Our group has earlier synthesized and investigated thionated LVX analogs, compounds 2 and 3, on A549 (non-small cell lung cancer) cell line and showed promising anticancer activity. The mechanism of cytotoxicity may be, in part, via aldehyde dehydrogenase enzyme inhibition and antioxidation. In this study, compounds 2 and 3 were evaluated on prostate (PC-3), breast (

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Yoon, Goo, Seung Hoon Cheon, Jung Hyun Shim, and Seung Sik Cho. "Design and Evaluation of Licochalcone A Derivatives as Anticancer Agents." Natural Product Communications 13, no. 6 (2018): 1934578X1801300. http://dx.doi.org/10.1177/1934578x1801300609.

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New derivatives of licochalcone A were synthesized and evaluated for their potential anticancer activities. Compounds 6 (( E)-N-(4-(3-(5-bromo-4-hydroxy-2-methoxy phenyl) acryloyl) phenyl)-4-isopropylbenzamide) and 8 (1-(3-dimethylamino-phenyl)-3-(2-trifluoromethyl-phenyl)-propenone) showed potent activity against the screened cancer cell lines with that of compound 6 ranging from 6.9 ± 0.2 μM to 22.9 ± 3.1 μM, and that of compound 8 from 4.2 ± 0.5 μM to 11.8 ± 0.7 μM. Both compounds showed stronger cytotoxicity than that of licochalcone A. These two candidates have very different substituents

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Saghdani, Nassima, Nabil El Brahmi, Abdelmoula El Abbouchi, et al. "Design, Synthesis, and Evaluation of EA-Sulfonamides and Indazole-Sulfonamides as Promising Anticancer Agents: Molecular Docking, ADME Prediction, and Molecular Dynamics Simulations." Chemistry 6, no. 6 (2024): 1396–414. http://dx.doi.org/10.3390/chemistry6060083.

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New EA-sulfonamides and indazole-sulfonamides were synthesized, characterized, and evaluated for their anticancer activities. The target compound structures were elucidated using various spectroscopic techniques such as NMR-{1H and 13C}, infrared spectroscopy, and high-resolution mass spectrometry. The anticancer activities of the novel compounds were evaluated against four human cancer cell lines, namely A-549, MCF-7, Hs-683, and SK-MEL-28 as well as the normal cell line HaCaT, using 5-fluorouracil and etoposide as reference drugs. Among the tested compounds, 9, 10, and 13 exhibited potent an

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Priolkar, Rudrax N. S., Sunil Shingade, Mahesh Palkar, and Shivalingrao M. Desai. "Design, Synthesis, and Characterization of Novel Linomide Analogues and their Evaluation for Anticancer Activity." Current Drug Discovery Technologies 17, no. 2 (2020): 203–12. http://dx.doi.org/10.2174/1570163815666181008151037.

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Background: According to WHO, in 2017, about 90.5 million people suffered from cancer and about 8.8 million deaths occurred due to disease. Although the chemotherapeutic agents have decreased the mortality among the cancer patients but high toxicity and non-specific targets are still major drawbacks. : Many researchers have identified linomide, a 4-hydroxy-2-quinolone derivative, as a lead molecule for the development of anticancer agents. With this background, we thought of the following objective. Objective: The objective of this research work involves the synthesis of a series of N-(2-(4- h

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Konyar, Dilan, Cenk A. Andac, and Erdem Buyukbingol. "Design, Synthesis and Cytotoxic Activity of Spiro(oxindole-3-3'- pyrrolidine) Derivatives." Letters in Drug Design & Discovery 15, no. 1 (2018): 37–45. http://dx.doi.org/10.2174/1570180814666170810120634.

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Background: Spiro[pyrrolidine-3,3'-oxindole] compounds are reported to be highly bioactive natural and synthetic products. Initially, spirooxindole alkaloids were isolated from plants of the Apocynaceae and Rubiaceae families, which were found to have a common scaffold, spiro[pyrrolidine-3,3'-oxindole], exhibiting anticancer activities., we specifically aimed at the synthesis, characterization and anticancer activity of novel spiro[pyrrolidine-3,3' -oxindole] derivatives, compounds 6a-c and 7. Methods: The synthesis was initiated by Knovenegal condensation of indole-2-one with an appropriate b

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OFLAZ, Feyza, Naz ÜNAL, Burcin GUNGOR, and Pakize CANTÜRK. "Evaluation of the Interactions of Cabozantinib with Topoisomerase Enzymes by in vitro Enzyme Activity Assays, and its Effects on Cancer Cell Proliferation." Cumhuriyet Science Journal 44, no. 4 (2023): 650–55. http://dx.doi.org/10.17776/csj.1376788.

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The discovery of many drugs in recent years provides a definitive solution in the treatment of various diseases, but today, despite the discovery of many effective anticancer drugs, there are various types of cancer that have limitations in treatment and are still not completely curable. Since most of these limitations are due to cancer cells gaining resistance or compounds only being effective in certain types of cancer cells, the search for more effective anticancer drugs that are also effective in these types of cancer is inevitable. Cabozantinib is in medical use as a highly effective anti

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Yang, Shu-Min, Qi-Shi Song, Chen Qing, Da-Gang Wu, and Xi-Kui Liu. "Anticancer Activity of Tirucallane Triterpenoids from Amoora dasyclada." Zeitschrift für Naturforschung C 61, no. 3-4 (2006): 193–95. http://dx.doi.org/10.1515/znc-2006-3-407.

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A new tetranortriterpene 3α-acetoxy-24,25,26,27-tetranortirucalla-7-ene-23(21)-lactone (3), and eleven other compounds were isolated from the twigs of Amoora dasyclada. The structure of compound 3 was identified on the basis of spectroscopic data, and the bioactive experiments of 1 and 3-5 against AGZY 83-a (human lung cancer cells) and SMMC-7721 (human liver cancer cells) are documented. Among them, compound 5 exhibited a strong activity against SMMC-7721.

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Chang, Chi-I., Cheng-Chih Hsieh, Yung-Shung Wein, et al. "Synthesis and Structure–Activity Relationship of Salvinal Derivatives as Potent Microtubule Inhibitors." International Journal of Molecular Sciences 24, no. 7 (2023): 6386. http://dx.doi.org/10.3390/ijms24076386.

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Salvinal is a natural lignan isolated from the roots of Salvia mitorrhiza Bunge (Danshen). Previous studies have demonstrated its anti-proliferative activity in both drug-sensitive and -resistant cancer cell lines, with IC50 values ranging from 4–17 µM. In this study, a series of salvinal derivatives was synthesized and evaluated for the structure–activity relationship. Among the twenty-four salvinal derivatives, six compounds showed better anticancer activity than salvinal. Compound 25 displayed excellent anticancer activity, with IC50 values of 0.13–0.14 µM against KB, KB-Vin10 (overexpress

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Suma, Artania Adnin Tri, Tutik Dwi Wahyuningsih, and Mustofa Mustofa. "Synthesis, Cytotoxicity Evaluation and Molecular Docking Studyof N-Phenylpyrazoline Derivatives." Indonesian Journal of Chemistry 19, no. 4 (2019): 1081. http://dx.doi.org/10.22146/ijc.45777.

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The synthesis of N-phenylpyrazolines 1-5 was performed by the cyclocondensation of phenylhydrazine and appropriate chalcones that have been synthesized from our previous work. All of the compounds were elucidated for their structure using GC-MS, FTIR, 1H, and 13C-NMR spectrometers. Their anticancer activity was evaluated against breast cancer cell line (T47D) and colorectal cancer cell line (WiDr). Compound 4 (4-(3-(4-chlorophenyl)-1-phenyl-4,5-dihydro-1H-pyrazol-5-yl)-2-methoxyphenol) was found to be the most potent compound with IC50 value of 13.11 µg/mL in T47D cell line and 3.29 µg/mL in W

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Hawash, Mohammed, Nidal Jaradat, Murad Abualhasan, et al. "Synthesis, chemo-informatics, and anticancer evaluation of fluorophenyl-isoxazole derivatives." Open Chemistry 19, no. 1 (2021): 855–63. http://dx.doi.org/10.1515/chem-2021-0078.

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Abstract The current study aimed to design and synthesize a novel series of fluorophenyl-isoxazole-carboxamide derivatives and evaluate their antiproliferative activities. Anticancer activities of the novel compounds were evaluated by MTS assay against four cancer cell lines, including liver (Hep3B, HepG2), cervical (HeLa), and breast (MCF-7), and α-fetoprotein tumor marker, cell cycle analysis, and annexin V tests. Chemo-informatics analysis showed that all synthesized derivatives 2a–2f obeyed Lipinski’s rule. Compound 2f was the most potent compound against Hep3B and Hep-G2 cancer cell lines

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Evren, Asaf Evrim, Leyla Yurttaş, Busra Eksellı, and Gulsen Akalın-Cıftcı. "Novel Tri-substituted Thiazoles Bearing Piperazine Ring: Synthesis and Evaluation of their Anticancer Activity." Letters in Drug Design & Discovery 16, no. 5 (2019): 547–55. http://dx.doi.org/10.2174/1570180815666180731122118.

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Background: Cancer cells are described as an unregulated growth and spread of abnormal cells. Recently, cancer has become the most important major reason for deaths in the world. Methods: For anticancer activity, we have used the MTT method and determine the early/late apoptosis by flow cytometry. Results: The title compounds were procured by reacting 2-chloro-N-[4-(pyridin-4-yl)thiazol-2- yl]acetamide with some substituted piperazine derivatives. The in vitro anticancer activity of synthesized compounds was tested against C6 rat glioma cells and A549 human lung carcinoma cells. As a result, t

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Sharma, Puja, Rajat Patel, Rohit R. Koshti, Akshay Vyas, and Chetan B. Sangani. "Synthesis, Biological Evaluation and Molecular Modeling of Novel Ethyl 2′-Amino-5′-oxo-1′- (4-phenylthiazol-2-yl)-2-(phenylthio)-1′,4′,5′,6′,7′,8′-hexahydro-[3,4′-biquinoline]-3′- carboxylate Derivatives and their Computational Quantum Mechanical Modelling." Asian Journal of Chemistry 35, no. 6 (2023): 1320–32. http://dx.doi.org/10.14233/ajchem.2023.27650.

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A new series of biquinoline-phenylthiazole hybrids were designed and synthesized by a base-catalyzed cyclocondensation through one-pot multicomponent reaction. All compounds were tested for in vitro antimicrobial and anticancer activities. Enzyme inhibitory activities of all compounds were carried out against FabH and EGFR. Majority of the synthesized compounds displayed promising antimicrobial as well as anticancer activity against used strains and cancer cell lines, respectively. All the compounds were tested for in vitro anticancer activities against two cancer cell lines A549 and Hep G2. C

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Racha, Hanumandlu, Balakishan Vadla, Kavitha Peddolla, and Sailu Betala. "Synthesis and Anticancer Activity of Novel Hetero Ring Fused Pyridine Amide Derivatives." Asian Journal of Chemistry 31, no. 11 (2019): 2485–91. http://dx.doi.org/10.14233/ajchem.2019.22150.

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A series of novel hetero ring fused pyridine amide derivatives were prepared starting from ethyl furo[2,3-b]pyridine-2-carboxylate (3) on reaction with ammonia to afford furo[2,3-b]pyridine-2-carboxamide (4), compound 4 on reaction with trifluoroacetic acid to give compound 5, which on reaction with bromoethyl acetate followed by hydrazine hydrate to give compound 7. Compound 7 when reacted with different substituted aromatic aldehydes to give Schiff base compounds (8a-l). Similarly, compound 6a when reacted with diverse substituted aliphatic amines to give amide derivatives (9a-h). All the sy

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Tan, Ayse, Ayse Sahin Yaglioglu, Nurhan Horasan Kishali, Ertan Sahin, and Yunus Kara. "Evaluation of Cytotoxic Potentials of Some Isoindole-1, 3-Dione Derivatives on HeLa, C6 and A549 Cancer Cell Lines." Medicinal Chemistry 16, no. 1 (2020): 69–77. http://dx.doi.org/10.2174/1573406415666181206115638.

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Objective: Considering this information, firstly, isoindole derivatives containing different functional groups 4-13 have been synthesized from 2-alkyl/aryl-3a, 4,7,7a-tetrahydro-1H-isoindole-1, 3(2H)-dione. Background: Norcantharimides are known as norcantharidine derivatives and contain an isoindole skeleton structure. Isoindole derivatives have positive effect on inflammatory pathologies including cancers. Methods: For the synthesis of all compounds, 2-alkyl/aryl-3a, 4,7,7a-tetrahydro-1H-isoindole- 1,3(2H)-dione was used as the starting compound. The syntheses were based on two main reaction

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Kumar, Satendra, and Himanshi Gupta. "Recent Development of Anticancer Agents." Journal of Phytopharmacology 11, no. 1 (2022): 17–23. http://dx.doi.org/10.31254/phyto.2022.11104.

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Cancer is the unwanted growth of the cell, which is developed trillion of the cells. It may be either Cancerous or Non-Cancerous. The aetiology involves the propagation of Cancer, defective DNA, or Mutation in DNA because of distinct Factors (Physical, Chemical, Biology, and Others). There is various kind of cancer (such as Carcinoma, Sarcoma, Myeloma, leukaemia and Lymphoma etc.). The sign and symptoms involve in Cancer (Such fever, loss of appetite, weight loss, thickening or lump in the body and unusual upset stomach or difficulty and swelling). Now a days the treatment is used in treatment

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Rizkuloh, Lina Rahmawati, Anindita Tri Kusuma Pratita, Mediana Mediana, and Anna Yuliana. "In silico study in toxicity parameters of Pigment Derivated Compounds of Monascus sp. mold as a cervical anti-cancer drugs candidate." Jurnal Teknologi Laboratorium 10, no. 2 (2021): 93–100. http://dx.doi.org/10.29238/teknolabjournal.v10i1.238.

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Toxicity prediction is very important for the development and design of new drugs because computational toxicity estimates are not only faster than the determination of toxic doses in animals, but can also help reduce the number of animal trials. The test uses pkCSM, Protox II, Toxtree, preADMET and T.E.S.T. From the results of research that has been carried out on 57 pigment derivated compounds of Monascus sp. mold, the results of the pkCSM application are 39 test compounds for the Protox-II application there is 1 compound, the Toxtree application produces 1 compound, for the PreADMET applica

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Gogoi, Barbi, and S. P. Saikia. "Virtual Screening and Network Pharmacology-Based Study to Explore the Pharmacological Mechanism of Clerodendrum Species for Anticancer Treatment." Evidence-Based Complementary and Alternative Medicine 2022 (November 2, 2022): 1–17. http://dx.doi.org/10.1155/2022/3106363.

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Background. Cancer is a second leading cause of death in the world, killing approximately 3500 per million people each year. Therefore, the drugs with multitarget pharmacology based on biological networks are crucial to investigate the molecular mechanisms of cancer drugs and repurpose the existing drugs to reduce adverse effects. Clerodendrum is a diversified genus with a wide range of economic and pharmacological properties. Limited studies were conducted on the genus’s putative anticancer properties and the mechanisms of action based on biological networks remains unknown. This study was ai

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Myrko, I. I., T. I. Chaban, V. V. Ohurtsov, I. V. Drapak, and V. S. Matiichuk. "Synthesis and study of the anticancer activity of some new 7H-[1,2,4]triazolo [3,4-b][1,3,4]thiadiazines." Current issues in pharmacy and medicine: science and practice 14, no. 3 (2021): 320–27. http://dx.doi.org/10.14739/2409-2932.2021.3.240361.

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The problem of finding effective low-toxic anticancer agents is one of the most important in modern medicine and pharmacy. Despite a large selection of anticancer drugs and a variety of mechanisms of their action, the effectiveness of existing drugs continues to be insufficient. Among the numerous natural and synthetic heterocyclic compounds that exhibit anticancer activity, 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives, which are able to initiate different pathways of tumor cell death. Based on this, the synthesis of new derivatives of this class of compounds and the study of their

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Goossens, Jean-François, Laurence Goossens, and Christian Bailly. "Hinokiflavone and Related C–O–C-Type Biflavonoids as Anti-cancer Compounds: Properties and Mechanism of Action." Natural Products and Bioprospecting 11, no. 4 (2021): 365–77. http://dx.doi.org/10.1007/s13659-021-00298-w.

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AbstractBiflavonoids are divided in two classes: C–C type compounds represented by the dimeric compound amentoflavone and C–O–C-type compounds typified by hinokiflavone (HNK) with an ether linkage between the two connected apigenin units. This later sub-group of bisflavonyl ethers includes HNK, ochnaflavone, delicaflavone and a few other dimeric compounds, found in a variety of plants, notably Selaginella species. A comprehensive review of the anticancer properties and mechanism of action of HNK is provided, to highlight the anti-proliferative and anti-metastatic activities of HNK and derivati

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Kitel, Radoslaw, Anna Byczek-Wyrostek, Katarzyna Hopko, Anna Kasprzycka, and Krzysztof Walczak. "Effect of Selected Silyl Groups on the Anticancer Activity of 3,4-Dibromo-5-Hydroxy-Furan-2(5H)-One Derivatives." Pharmaceuticals 14, no. 11 (2021): 1079. http://dx.doi.org/10.3390/ph14111079.

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The pharmacological effects of carbon to silicon bioisosteric replacements have been widely explored in drug design and medicinal chemistry. Here, we present a systematic investigation of the impact of different silyl groups on the anticancer activity of mucobromic acid (MBA) bearing furan-2(5H)-one core. We describe a comprehensive characterization of obtained compounds with respect to their anticancer potency and selectivity towards cancer cells. All four novel compounds exert stronger antiproliferative activity than MBA. Moreover, 3b induce apoptosis in colon cancer cell lines. A detailed i

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Almalki, Abdulraheem S. A., Syed Nazreen, Azizah M. Malebari, et al. "Synthesis and Biological Evaluation of 1,2,3-Triazole Tethered Thymol-1,3,4-Oxadiazole Derivatives as Anticancer and Antimicrobial Agents." Pharmaceuticals 14, no. 9 (2021): 866. http://dx.doi.org/10.3390/ph14090866.

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A library of 1,2,3-triazole-incorporated thymol-1,3,4-oxadiazole derivatives (6–18) hasbeen synthesized and tested for anticancer and antimicrobial activities. Compounds 7, 8, 9, 10, and 11 exhibited significant antiproliferative activity. Among these active derivatives, compound 2-(4-((5-((2-isopropyl-5-methylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol (9) was the best compound against all three tested cell lines, MCF-7 (IC50 1.1 μM), HCT-116 (IC50 2.6 μM), and HepG2 (IC50 1.4 μM). Compound 9 was found to be better than the standard drugs, doxorubicin and 5-f

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