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Journal articles on the topic 'Cytotoxic compound'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

Hamed, Fadil M., and Mohammad H. Mohammad. "Synthesis ,Characterization and invitro evaluation of anticancer activity of new hydroxamicacid basedHDACi containing substituted thaizolesas a cap linking moiety." JOURNAL OF ADVANCES IN CHEMISTRY 13, no. 10 (2017): 5954–61. http://dx.doi.org/10.24297/jac.v13i10.5886.

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The present study was undertaken to synthesize, characterize and evaluate the anticancer activity of new derivatives of hydroxamate â€“based HDACi having S-subistituted-5-amino1,3,4thadiazole as a cap linking moiety ,with suitable aliphatic linker.The structures and purity of the targeted compounds were confirmed by TLC , FTIR ,H-NMR and mass spectroscopy and their anticancer activity were evaluated by comparative cytotoxic study , Using HeLa nuclear extract and normal embryonic fibroblasts cell lines.All the synthesized compounds shows good anticancer activity, represented by their high rate

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2

Maher, Mai, Asmaa E. Kassab, Ashraf F. Zaher, and Zeinab Mahmoud. "Novel Pyrazolo[3,4-d]pyrimidines as Potential Cytotoxic Agents: Design, Synthesis, Molecular Docking and CDK2 Inhibition." Anti-Cancer Agents in Medicinal Chemistry 19, no. 11 (2019): 1368–81. http://dx.doi.org/10.2174/1871520619666190417153350.

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Background: Pyrazolo[3,4-d]pyrimidine scaffold was reported to possess potent cytotoxic and CDK2 inhibitory activity as analogue of roscovitine. Objective: To design and synthesize novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidine derivatives as bioisosters of roscovitine with potential cytotoxic and CDK2 inhibitory activity. Methods: A series of novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidines were designed and synthesized. Structural elucidation for all the newly synthesized compounds was achieved through performing MS, 1H NMR, 13C NMR and IR spectral techniques. Eight compounds were scree

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3

Manzo, Lawaly Maman, Yijuan Cheng, Ling Yang, et al. "Small-scale screening program for the identification of cytotoxic Oxazolo[5,4-d]pyrimidine derivatives based on Whole Cell Viability Assay." Indian Journal of Pharmaceutical and Biological Research 3, no. 02 (2015): 58–65. http://dx.doi.org/10.30750/ijpbr.3.2.6.

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For over last couple of decades, there has been a robust activity aimed towards the discovery of novel anti-cancer therapeutics. An approach to identify starting points for new drug candidates is high throughput screening of compound library collection. In this work, we describe the application of a Tetrazolium-based, 96-well small scale screening assay to screen a mini library of 19 compounds bearing Oxazolo[5,4-d]pyrimidine structures against human umbilical vein endothelial cells. Primary actives identified against HUVEC were retested and the IC50 value compounds were estimated for HUVEC. T

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4

Nabil, Sara, and Abeer Obaid Al-Dossary. "in vitro Cytotoxic Evaluation of Some New Synthesized Pyridazine Derivatives." Asian Journal of Chemistry 31, no. 3 (2019): 744–50. http://dx.doi.org/10.14233/ajchem.2019.21832.

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A series of novel pyridazine, pyrazoles, pyrimidines derivatives have been synthesized through the reaction of chloropyridazine (1) with p-phenylenediamine to give compound 2. Diazotization of compound 2 followed by coupling with active methylene compounds namely acetylacetone, ethylcyanoacetate and/or ethylacetoacetate afforded novel hydrazons derivatives (4-6). The resulting hydrazons can have been cyclized using hydrazine hydrate and guanidine gave the corresponding pyrazoles (7-9) and pyimidine (10) derivatives. Reaction of compound 2 with acrylonitrile, aromatic aldehyde, p-chloroacetophe

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5

Sirka, Lütfiye, Hacer Doğan, Mehmet Refik Bahar, et al. "(E)-1-(4-Hydroxyphenyl)-3-(substituted-phenyl) prop-2-en-1-ones: Synthesis, In Vitro Cytotoxic Activity and Molecular Docking Studies." Acta Chimica Slovenica 69, no. 2 (2022): 281–92. http://dx.doi.org/10.17344/acsi.2021.7080.

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A series of chalcone compounds (2–11) were designed and synthesized to determine their cytotoxic effects. The structures of 2–11 were fully characterized by their physical and spectral data. The in vitro cytotoxic effects of 2–11 were evaluated against human ovarian cancer (A2780), breast cancer (MCF-7) and prostate cancer (PC-3 and LNCaP) cell lines. The activity potentials of compounds were further evaluated through molecular docking studies with AutoDock4 and Vina softwares. All the compounds (except compound 5) showed significant cytotoxic effects at high doses in all cancer cell lines. Am

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6

Hussain, Fahad, Fahad Imtiaz Rahman, Poushali Saha, et al. "Synthesis of Sugar and Nucleoside Analogs and Evaluation of Their Anticancer and Analgesic Potentials." Molecules 27, no. 11 (2022): 3499. http://dx.doi.org/10.3390/molecules27113499.

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Chemical modification of sugars and nucleosides has a long history of producing compounds with improved selectivity and efficacy. In this study, several modified sugars (2–3) and ribonucleoside analogs (4–8) have been synthesized from α-d-glucose in a total of 21 steps. The compounds were tested for peripheral anti-nociceptive characteristics in the acetic acid-induced writhing assay in mice, where compounds 2, 7, and 8 showed a significant reduction in the number of writhes by 56%, 62%, and 63%, respectively. The compounds were also tested for their cytotoxic potential against human HeLa cell

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7

Polokhina, K. V., D. E. Kytova, A. V. Shtemenko, and N. I. Shtemenko. "Cytotoxic activity of the cluster rhenium compound with ?-alanine ligands." Ukrainian Biochemical Journal 92, no. 1 (2020): 120–26. http://dx.doi.org/10.15407/ubj92.01.120.

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8

Acar Çevik, Ulviye, Begüm Nurpelin Sağlık, Cankız Mina Ardıç, Yusuf Özkay, and Özlem Atlı. "Synthesis and evaluation of new benzimidazole derivatives with hydrazone moiety as anticancer agents." Turkish Journal of Biochemistry 43, no. 2 (2018): 151–58. http://dx.doi.org/10.1515/tjb-2017-0167.

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Abstract Objectives: Cancer is one of the leading causes of death throughout the world. Current therapy options suffer from the major limitations of side effects and drug resistance. Thus, continuing search for newer and safer anticancer drugs remains critically important. From this point of view, in the present study benzimidazole-hydrazone derivatives were synthesized by aiming at the identification of new chemical entities as potent anticancer agents. Material and methods: A series of 12 new compounds of 4-(5(6)-substituted-1H-benzimidazol-2-yl)-N′thiophen/furan-2-yl-methylene) benzohydrazi

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9

Huo, Shaojie, Jichun Wu, Xicheng He, Lutai Pan, and Jiang Du. "Two New Cytotoxic Steroidal Alkaloids from Sarcococca Hookeriana." Molecules 24, no. 1 (2018): 11. http://dx.doi.org/10.3390/molecules24010011.

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Two new steroidal alkaloids, named hookerianine A (1) and hookerianine B (2) were isolated from the stems and roots of Sarcococca hookeriana Baill., along with two known compounds, sarcorucinine G (3) and epipachysamine D (4). On the basis of spectroscopic methods and by comparison with literature data, their structures were determined. As well as X-ray crystallography was performed to confirm compound 4. To identify novel antitumor inhibitors, all compounds were performed a CCK-8 assay against five human cancer cell lines SW480, SMMC-7721, PC3, MCF-7 and K562 in vitro. Compound 2 exhibited mo

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10

Sary, Hanan G., Abdel Nasser B. Singab, and Khaled Y. Orabi. "New Cytotoxic Guaianolides from Centaurea Aegyptiaca." Natural Product Communications 11, no. 6 (2016): 1934578X1601100. http://dx.doi.org/10.1177/1934578x1601100603.

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The ethanol extract of Centaurea aegyptiaca aerial parts afforded two new chlorinated bioactive guaianolides, cenegyptin A (1) and cenegyptin B (2), in addition to four known sesquiterpenes (3-6). Their identities were established on the basis of their spectral data. The cytotoxicity (IC50, μM) of compounds 1-6 were evaluated against hepatic (HEPG2) and laryngeal (HEP2) carcinoma cell lines in comparison with normal fibroblasts (BHK). Compound 1 showed cytotoxic activity against HEPG2 and HEP2 with IC50 values of 7.2 ± 0.04 and 7.5 ± 0.02, respectively. However, compound 2 exhibited only a lim

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11

Ahunun, I. Frances. "Comparative Cytotoxic Assay of Pharmaceutical Drug Compounds." Journal of Pharma and Drug Regulatory Affairs 1, no. 2 (2019): 15–18. https://doi.org/10.5281/zenodo.3247270.

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<em>The drug compounds under assay have been previously employed for the treatment of restenosis and other diabetic complications. They show potential for the treatment of diseases such as rheumatoid arthritis, atherosclerosis, cirrhosis, fibrosis, cancer and autoimmune diseases. The cytotoxicity of these compounds have been established, however this study brings all three compounds together for a comparative analysis. The importance of research work into cancer treatment cannot be overemphasized with the annual incidence of mortality due to the disease. This study is done in hindsight, bringi

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12

Heise, Niels V., Toni C. Denner, Selina Becker, Sophie Hoenke, and René Csuk. "Developing an Amide-Spacered Triterpenoid Rhodamine Hybrid of Nano-Molar Cytotoxicity Combined with Excellent Tumor Cell/Non-Tumor Cell Selectivity." Molecules 28, no. 17 (2023): 6404. http://dx.doi.org/10.3390/molecules28176404.

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Asiatic acid, a pentacyclic triterpene, was converted into a series of piperazinyl, homopiperazinyl, and 1,5-diazocinyl spacered rhodamine conjugates, differing in the type of spacer and the substitution pattern on the rhodamine moiety of the hybrids. The compounds were tested for cytotoxic activity in SRB assays and compound 12, holding an EC50 of 0.8 nM, was the most cytotoxic compound of this series, but compound 18 (containing a ring expanded 1,5-diazocinyl moiety and n-propyl substituents on the rhodamine) was the most selective compound exhibiting a selectivity factor of almost 190 while

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13

Mayanti, Tri, Zulfikar, Sarah Fawziah, et al. "New Triterpenoids from Lansium domesticum Corr. cv kokossan and Their Cytotoxic Activity." Molecules 28, no. 5 (2023): 2144. http://dx.doi.org/10.3390/molecules28052144.

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Lansium domesticum Corr. is a member of the Meliaceae family that is widely spread in tropical and subtropical region of Asia and America. Traditionally, the fruit of this plant has been consumed because of its sweet taste. However, the fruit peels and the seeds of this plant have been rarely utilized. The previous chemical investigation of this plant showed the presence of secondary metabolites with many biological activities, including cytotoxic triterpenoid. Triterpenoids is a class of secondary metabolites which contain thirty carbon atoms in the main skeleton. The high modification of thi

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14

León-González, Antonio J., Miguel López-Lázaro, José L. Espartero, and Carmen Martín-Cordero. "Cytotoxic Activity of Dihydrochalcones Isolated from Corema Album Leaves against HT-29 Colon Cancer Cells." Natural Product Communications 8, no. 9 (2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800918.

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During our search for cytotoxic compounds from Andalusian vascular plants, the ethyl acetate extract from the leaves of Corema album (L.) D. Don (Ericaceae) was selected for its cytotoxic activity against the HT-29 human colon adenocarcinoma cell line. Two dihydrochalcones, 2′,4′-dihydroxydihydrochalcone (1) and 2′-methoxy-4′-hydroxydihydrochalcone (2), have been isolated from the leaves of C. album. Their structural identification was based on 1H NMR and 13C NMR data, including 2D NMR, and mass spectrometry. These compounds were subjected to the sulfhorhodamine B (SRB) cytotoxic assay against

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15

Cao, Thao Quyen, Bo Mi Lee, Yeon Woo Jung, Van Thu Nguyen, Jeong Ah Kim, and Byung Sun Min. "Cytotoxic Activity of Compounds from Styrax obassia." Natural Product Communications 12, no. 2 (2017): 1934578X1701200. http://dx.doi.org/10.1177/1934578x1701200230.

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Cancer is a major public health burden in both developed and developing countries. Plant-derived compounds have played an important role in the development of useful anti-cancer agents. The current study was designed to evaluate the cytotoxic activity of chemical compounds from the stem bark of Styrax obassia. Seven known compounds (1–7) were isolated and identified. Compound 2 exhibited cytotoxic activity against the breast cancer cell line MCF-7 with an IC50 of 27.9 μM, followed by the human cervical cancer cell line Hela with an IC50 of 23.3 μM, and the human promyelocytic leukemia cell lin

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16

Kandeel, Manal M., Mohamed Kamal AbdElhameid, Mohamed Adel, Muhammad Y. Al-Shorbagy, and Ahmed T. Negmeldin. "Design, Synthesis, and Cytotoxicity Evaluation of Novel Indolin-2-One Based Molecules on Hepatocellular Carcinoma HepG2 Cells as Protein Kinase Inhibitors." Molecules 30, no. 5 (2025): 1105. https://doi.org/10.3390/molecules30051105.

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A series of indolinone-based derivatives were designed and synthesized using the hybrid pharmacophoric design approach as cytotoxic kinase inhibitors. The cytotoxic effects of the designed molecules were tested against MCF-7 and HepG-2 cell lines. Compounds 9 and 20 were the most cytotoxic, with IC50 values against HepG-2 and MCF-7 cells ranging from 2.53 to 7.54 µM. Additionally, compounds 9 and 20 were also found to be slightly more cytotoxic than indirubin with 2.2–2.7-fold higher cytotoxicity with HepG-2 cells. CDK-2 and CDK-4 kinase enzyme inhibition assay showed that compound 9 had a hig

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17

Fadhli, Haiyul, Wıky Rahmayanı, Regina Allaya, Ikhsal Mukri Jumadila, Armon Fernando, and Rahayu Utami. "Cytotoxic activity of isolate compounds from derendan (Lansium parasiticum (Osbeck) K.C. Sahni & Bennet) fruit peel." JURNAL ILMU KEFARMASIAN INDONESIA 22, no. 1 (2024): 15. http://dx.doi.org/10.35814/jifi.v22i1.1309.

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Derendan (Lansium parasiticum (Osbeck) K.C. Sahni & Bennet) is a plant from the Meliaceae family that grows in the tropics, especially in Sumatra (Indonesia). It was reported that this plant has antimalarial, antimutagenic, and anticancer properties. This study aims to determine the cytotoxic activity of compounds isolated from the methanol extract of Lansium parasiticum bark. Extraction using maceration method with methanol solvent. Vacuum Liquid Chromatography (KVC) with 21 different eluent ratios (n-hexane : ethyl acetate and ethyl acetate ; methanol) was utilized for the fractionation.

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18

Jing, Songsong, Zhuo Qu, Chengcheng Zhao, et al. "Dihydroisocoumarins and Dihydroisoflavones from the Rhizomes of Dioscorea collettii with Cytotoxic Activity and Structural Revision of 2,2′-Oxybis(1,4-di-tert-butylbenzene)." Molecules 26, no. 17 (2021): 5381. http://dx.doi.org/10.3390/molecules26175381.

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The investigation of the constituents of the rhizomes of Dioscorea collettii afforded one new dihydroisocoumarin, named (−)-montroumarin (1a), along with five known compounds—montroumarin (1b), 1,1′-oxybis(2,4-di-tert-butylbenzene) (2), (3R)-3′-O-methylviolanone (3a), (3S)-3′-O-methylviolanone (3b), and (RS)-sativanone (4). Their structures were elucidated using extensive spectroscopic methods. To the best of our knowledge, compound 1a is a new enantiomer of compound 1b. The NMR data of compound 2 had been reported but its structure was erroneous. The structure of compound 2 was revised on the

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19

Setyowati, Erna Prawita, Sudarsono Sudarsono, and Retno Murwanti. "Penares sp sponge from Menjangan Island-water West Bali National Park: Isolation of Cytotoxic Compounds." Majalah Obat Tradisional 22, no. 3 (2017): 153. http://dx.doi.org/10.22146/mot.31547.

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Sponges are multicellular animals which have cytotoxic compounds. In this study, isolation and cytotoxic activity of Penares sp sponge from Menjangan island-water West Bali National Park have been carried out. The results showed that chloroform extract and GF V Penares sp fraction were toxic according to Brine Shrimp Lethality Test method (each 85% and 63.3% mortality at 25μg/mL concentration). The isolation result of GF V fraction was obtained a compound (Spot 4) that is active as cytotoxic agent against T47D cells (IC50 of 12.7 ug/mL). Spot 4 is a terpenoid compound which has conjugated doub

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20

Liu, Zhen-Zhen, Jun-Cheng Ma, Peng Deng, Fu-Cai Ren, and Ning Li. "Chemical Constituents of Thesium chinense Turcz and Their In Vitro Antioxidant, Anti-Inflammatory and Cytotoxic Activities." Molecules 28, no. 6 (2023): 2685. http://dx.doi.org/10.3390/molecules28062685.

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Three novel compounds (1–3) along with twenty-six known compounds, two known steroids (4–5) and twenty-four known phenylpropanoids (6–29) were isolated from the whole plant of Thesium chinense Turcz. The structures of the three new compounds were elucidated on the basis of ESI-MS, HR-ESIMS, 1D and 2D NMR, IR, UV spectroscopic data. The absolute stereochemistry of compound 1 was determined by the Gauge-Including Atomic Orbitals (GIAO) method. The in vitro antioxidant, anti-inflammatory and cytotoxic activities of the isolated compounds were evaluated by DPPH radical-scavenging assay, LPS-activa

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21

Darmawan, Akhmad, Maulidiyah Maulidiyah, Megawati Megawati, et al. "Cytotoxic of Usnic Acid Isolated from Ramalina sp." Journal of Tropical Life Science 14, no. 02 (2024): 349–56. http://dx.doi.org/10.11594/jtls.14.02.14.

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Ramalina sp. (Ramalinaceae) is a type of lichen known to contain many active secondary metabolite compounds that have the potential to be used as medicine or medicinal raw materials. One of the biological activities possessed by Ramalina sp. lichen is its anticancer activity. This research aims to isolate and identify active secondary metabolite compounds from the methanol extract of the Ramalina sp. lichen and to find out the cytotoxic activity of the isolated compound against MCF7 breast cancer cells. Compound 1 (usnic acid) was successfully isolated from fraction A. The isolation and purifi

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22

Xiao, Kun-Min, Jun-Ming Wang, Ling-Yun Zhou, et al. "Cytotoxic Triterpenes From Trametes orientalis." Natural Product Communications 15, no. 5 (2020): 1934578X2092162. http://dx.doi.org/10.1177/1934578x20921621.

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One new triterpene, 24-ene-2′-methyl carboxy acetylquercinicate, and 3 known compounds were isolated from the ethyl acetate extract of the fruiting bodies of Trametes orientalis (Yasuda) Imazeki. Their structures were elucidated by means of extensive spectroscopic analysis and compared with data reported in the literature. Furthermore, they were evaluated for their cytotoxicity against 5 human cancer cell lines in vitro. Compound 4 showed significant cytotoxicity, especially to the leukemic HL-60 cell line (IC50 = 1.77 ± 0.07 μM), while compounds 1-3 showed significant cytotoxicity to SMMC-772

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23

Rodrigo, Mellisa. "Compounds 7-Hydroxy-6-Metoxic Cytotoxic Cytotoxic Stem Leather From Chisochetonmacrophyllus (Meliaceae) Bark." International Journal of Science and Society 2, no. 2 (2020): 363–67. http://dx.doi.org/10.54783/ijsoc.v2i2.180.

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A phenyl propanoid compound, 7-hydroxy-6-methoxycoumarin has been isolated from the bark of Chisocheton macrophyllus (Meliaceae). The chemical structure of isolated compound was identified on the basis of spectroscopic data including UV, IR, 1D-NMR, 2D-NMR and mass along with comparison with those spectral data previously reported. 7-hydroxy-6-methoxycoumarin compound showed cytotoxic effect against P-388 murine leukemia cell with IC50 value of 16.5 mg/mL. 7-hydroxy-6-methoxycoumarin compound was reported for the first time from genus of Chisocheton.

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Rodrigo, Mellisa. "Compounds 7-Hydroxy-6-Metoxic Cytotoxic Cytotoxic Stem Leather From Chisochetonmacrophyllus (Meliaceae) Bark." International Journal of Science and Society 2, no. 2 (2020): 363–67. http://dx.doi.org/10.54783/ijsoc.v2i2.180.

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A phenyl propanoid compound, 7-hydroxy-6-methoxycoumarin has been isolated from the bark of Chisocheton macrophyllus (Meliaceae). The chemical structure of isolated compound was identified on the basis of spectroscopic data including UV, IR, 1D-NMR, 2D-NMR and mass along with comparison with those spectral data previously reported. 7-hydroxy-6-methoxycoumarin compound showed cytotoxic effect against P-388 murine leukemia cell with IC50 value of 16.5 mg/mL. 7-hydroxy-6-methoxycoumarin compound was reported for the first time from genus of Chisocheton.

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25

Milawati, Hersa, Winda Sukmawati, Desi Harneti, et al. "Cytotoxic Sesquiterpenoids from the Stem Bark of Aglaia harmsiana (Meliaceae)." Indonesian Journal of Chemistry 20, no. 6 (2020): 1448. http://dx.doi.org/10.22146/ijc.47808.

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Three aromadendrane-type sesquiterpenoids, spathulenol (1), 4β,10α-dihydroxyaromadendrane (2), and 4α,10α-dihydroxyaromadendrane (3) were isolated from the stem bark of Aglaia harmsiana (Meliaceae). Compound 3 was isolated for the first time from Aglaia genus. The chemical structures of isolated compounds were elucidated by various spectroscopic methods, including one and two-dimensional NMR, as well as mass spectroscopy analysis. These sesquiterpenoids 1-3 were evaluated for their cytotoxic activity against MCF-7 breast cancer cell lines. The IC50 value of compound 1-3 were 31.65 ± 0.1, 8.41

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26

Kishk, Safaa M., Enas E. Eltamany, Mohamed S. Nafie, et al. "Design and Synthesis of Coumarin Derivatives as Cytotoxic Agents through PI3K/AKT Signaling Pathway Inhibition in HL60 and HepG2 Cancer Cells." Molecules 27, no. 19 (2022): 6709. http://dx.doi.org/10.3390/molecules27196709.

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In this study, a series of coumarin derivatives, either alone or as hybrids with cinnamic acid, were synthesized and evaluated for their cytotoxicity against a panel of cancer cells using the MTT assay. Then, the most active compounds were inspected for their mechanism of cytotoxicity by cell-cycle analysis, RT-PCR, DNA fragmentation, and Western blotting techniques. Cytotoxic results showed that compound (4) had a significant cytotoxic effect against HL60 cells (IC50 = 8.09 µM), while compound (8b) had a noticeable activity against HepG2 cells (IC50 = 13.14 µM). Compounds (4) and (8b) mediate

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Galassi, Rossana, Nicola Sargentoni, Sofia Renzi, et al. "Anticancer Activity of Imidazolyl Gold(I/III) Compounds in Non-Small Cell Lung Cancer Cell Lines." Pharmaceuticals 17, no. 9 (2024): 1133. http://dx.doi.org/10.3390/ph17091133.

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Lung cancer is a leading cause of cancer-related death worldwide that needs updated therapies to contrast both the serious side effects and the occurrence of drug resistance. A panel of non-small cell lung cancer (NSCLC) cells were herein employed as cancer models. Eight structurally related gold(I) and gold(III) complexes with NHC and halides or triphenylphosphane ligands were investigated as lung cancer cell growth inhibitors. As expected, gold compounds with PPh3 were found to be more cytotoxic than homoleptic [(NHC)2-Au(I)]X or heteroleptic NHC-Au(I)X or NHC-Au(III)X3 complexes. Mixed liga

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28

Castro, Jessica, Marlon Bravo, Meritxell Albertí, et al. "Dinuclear Iron Complexes of Iminopyridine-Based Ligands as Selective Cytotoxins for Tumor Cells and Inhibitors of Cancer Cell Migration." Pharmaceutics 14, no. 12 (2022): 2801. http://dx.doi.org/10.3390/pharmaceutics14122801.

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A family of dinuclear iron (II) compounds with iminopyridine-based ligands displays selective cytotoxic activity against cancer cell lines. All compounds have IC50 values 2–6 fold lower than that of cisplatin, and 30–90 fold lower than that of carboplatin for the tumor cell lines assayed. Comparing the IC50 values between tumor and non-tumor cell lines, the selectivity indexes range from 3.2 to 34, compound 10, [Fe2(4)2(CH3CN)4](BF4)4, showing the highest selectivity. Those compounds carrying substituents on the iminopyridine ring show the same cytotoxicity as those without substituents. Howev

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29

Yu, Hao-Bing, Xiao-Li Wang, Wei-Heng Xu, et al. "Eutypellenoids A–C, New Pimarane Diterpenes from the Arctic Fungus Eutypella sp. D-1." Marine Drugs 16, no. 8 (2018): 284. http://dx.doi.org/10.3390/md16080284.

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Three new pimarane diterpenes, eutypellenoids A–C (1–3), together with a known compound, eutypenoid C (4), were isolated from the culture extract of Eutypella sp. D-1 derived from the Arctic region. Compounds 1–3 possessed an uncommon tetrahydrofuran-fused pimarane diterpene skeleton. The structures of all compounds were determined by detailed spectroscopic analysis, electronic circular dichroism (ECD) analysis, as well as a comparison with the literature data. Antibacterial, antifungal, and cytotoxic activities of these compounds were evaluated. Compound 2 displayed antibacterial activity aga

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30

Viriyaadhammaa, Natsima, Aroonchai Saiai, Waranya Neimkhum, et al. "Cytotoxic and Antiproliferative Effects of Diarylheptanoids Isolated from Curcuma comosa Rhizomes on Leukaemic Cells." Molecules 25, no. 22 (2020): 5476. http://dx.doi.org/10.3390/molecules25225476.

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Curcuma comosa belongs to the Zingiberaceae family. In this study, two natural compounds were isolated from C. comosa, and their structures were determined using nuclear magnetic resonance. The isolated compounds were identified as 7-(3,4-dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene (1) and trans-1,7-diphenyl-5-hydroxy-1-heptene (2). Compound 1 showed the strongest cytotoxicity effect against HL-60 cells, while its antioxidant and anti-inflammatory properties were stronger than those of compound 2. Compound 1 proved to be a potent antioxidant, compared to ascorbic acid. Neither compounds

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Saeedian Moghadam, Ebrahim, Farhad Saravani, Seyednasser Ostad, Shohreh Tavajohi, Morteza Pirali Hamedani, and Mohsen Amini. "Design, synthesis and cytotoxicity evaluation of indibulin analogs." Heterocyclic Communications 24, no. 4 (2018): 211–17. http://dx.doi.org/10.1515/hc-2018-0016.

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AbstractIndibulin is one of the most potent tubulin polymerization inhibitors with minimal peripheral neuropathy. The design and synthesis of new indibulin analogs were carried out in order to investigate their anti-cancer activity. The target compounds 4a–i were synthesized in multistep reactions starting with the related indole derivatives. Compound 4f shows the highest cytotoxic activity on HT-29 and Caco-2 cell lines with the respective half maximal inhibitory concentration (IC50) values of 5.1 μm and 7.3 μm. In the case of the T47-D cell line, compound 4c exerts the best cytotoxic activit

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32

Mohamed, Gamal A., Ali A. Alqarni, Hossam M. Abdallah, Abdelsattar M. Omar, and Sabrin RM Ibrahim. "Cytotoxic and alpha amylase-inhibitory metabolites from Tagetes minuta: In vitro evaluation and docking studies." Tropical Journal of Pharmaceutical Research 22, no. 4 (2023): 795–804. http://dx.doi.org/10.4314/tjpr.v22i4.12.

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Purpose: To investigate the cytotoxic and alpha-amylase inhibitory (AAI) potential of methanol (MeOH) extract of T. minuta and its isolated metabolites.  Methods: Phytochemical investigation of MeOH extract of the aerial parts of T. minuta was accomplished using SiO2 and Rp-18 column chromatography (CC). The structures of the isolated metabolites were determined and verified based on various data, in addition to comparison with literature data. The metabolites were assessed for cytotoxic potential against HepG2, MCF-7, and HCT116 cell lines utilizing sulphur rhodamine B (SRB) assay. The

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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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Supratman, Unang, Samuel San Parulian, Nurlelasari Nurlelasari, et al. "Sesquiterpenoids from Stem Bark of Chisocheton lasiocarpus and Their Cytotoxic Activity against MCF-7 Breast Cancer Cell." Molekul 17, no. 3 (2022): 413. http://dx.doi.org/10.20884/1.jm.2022.17.3.6425.

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Sesquiterpenoids are derivatives of terpenoid compound that have a diverse skeleton and broad spectrum of biological activities, particularly anticancer activity. This research reported the isolation and elucidation structure of sesquiterpenoid from Chisocheton lasiocarpus stem bark, as well as their cytotoxic activity. Four sesquiterpenoid compounds, namely eudesm-4(15)-ene-1β,6β-diol (1), allo-aromadendrane-10α,14-diol (2), allo-aromadendrane-10β,14-diol (3) and guaianediol (4), were isolated for the first time from Chisocheton lasiocarpus stem bark. The chemical structure of all compounds w

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Mohammed, Jalal Hassan, and Saadon Abdulla Aowda. "Cytotoxic Activity of New Thiol Derivatives." International Journal of Drug Delivery Technology 10, no. 02 (2020): 244–49. http://dx.doi.org/10.25258/ijddt.10.2.10.

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This research included synthesized ten new compounds (1–10) based on alkyl halides, and estimated their anti-cancer effectiveness. All prepared products are proven by Proton nuclear magnetic resonance (1H NMR) and infrared spectroscopy (IR). The anti-cancer effect of compounds 6, 9, and 10 were assessed on MCF-7 breast cancer in human cells, then WRL68 cancer cells. Compound 9 revealed to be most strong with IC50 119.2 μg/mL against MCF-7, while other compounds showed moderate anti-cancer activity. The discoveries of ponder can upgrade the understood of natural exercises of these thiols compou

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Hamada, Toshiyuki, Yoshito Matsumoto, Chin-Soon Phan, et al. "Aaptamine-Related Alkaloid from the Marine Sponge Aaptos aaptos." Natural Product Communications 14, no. 9 (2019): 1934578X1986393. http://dx.doi.org/10.1177/1934578x19863935.

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A new aaptamine-related alkaloid, 1,3-dioxolo [4,5- d] benzo [ de]-1,6-naphthyridine (methylenedioxyaaptamine, 1), was isolated from the organic extracts of the Bornean marine sponge Aaptos aaptos, together with a known aaptamine derivative, 8,9,9-trimethoxy-9 H-benzo [ de]-1,6-naphthyridine (2). The structure of compound 1 was elucidated by interpretation of its spectroscopic data. Two compounds were tested for their cytotoxic potentials against adult T-cell leukemia (ATL) cells, and compound 1 showed moderate cytotoxic potential.

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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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Liang, Chong, Chonglun Zhang, Yinlin Zhuo, Baocheng Gong, Weizhuo Xu, and Guogang Zhang. "1,5,6-Trimethoxy-2,7-dihydroxyphenanthrene from Dendrobium officinale Exhibited Antitumor Activities for HeLa Cells." International Journal of Molecular Sciences 24, no. 20 (2023): 15375. http://dx.doi.org/10.3390/ijms242015375.

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Natural products are irreplaceable reservoirs for cancer treatments. In this study, 12 phenanthrene compounds were extracted and isolated from Dendrobium officinale. Each chemical structure was identified using comprehensive NMR analysis. All compounds were evaluated for their cytotoxic activities against five tumor cell lines, i.e., HeLa, MCF-7, SK-N-AS, Capan-2 and Hep G2. Compound 5, 1,5,6-trimethoxy-2,7-dihydroxyphenanthrene, displayed the most significant cytotoxic effect against HeLa and Hep G2 cells, with an IC50 of 0.42 and 0.20 μM. For Hela cells, further experiments demonstrated that

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Vu, Vu Van, Trinh Thi Nhung, Nguyen Thi Thanh, et al. "Synthesis and Biological Evaluation of New (−)-Gossypol-Derived Schiff Bases and Hydrazones." Journal of Chemistry 2017 (2017): 1–8. http://dx.doi.org/10.1155/2017/3687182.

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A series of 14 new (-)-gossypol Schiff bases and hydrazones have been synthesized via an in situ procedure in high yields. Structural data showed that all target compounds exist as the enamine tautomer. Bioassays showed that several compounds exhibited cytotoxic effects against three human cancer cell lines. Compound 8a showed the greatest cytotoxic effect against hepatocellular carcinoma (HepG2), lung carcinoma (LU-1), and breast cancer (MCF-7) cell lines with IC50 values of 20.93, 13.58, and 9.40 μM, respectively. However, in an antibacterial test, compounds 8a and 8b inhibited Staphylococcu

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Alagöz, Mehmet Abdullah, Arzu Karakurt, Ceylan Hepokur, et al. "Synthesis of New 1-Aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone Oxime Ether Derivatives and Investigation of Their Cytotoxic Effects." Processes 9, no. 11 (2021): 2019. http://dx.doi.org/10.3390/pr9112019.

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In this study, 12 new 1-aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone oxime ether derivatives were designed and synthesized to investigate their cytotoxic effects. The in vitro cytotoxic activities of the compounds were evaluated against cervix, colon, breast, glioma, neuroblastoma, and lung cancer cell lines, as well as a healthy cell line using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide (MTT) assays with 5-fluorouracil (5-FU) as the reference compound. Compound 5f (IC50 = 5.13 µM) was found to be more effective than 5-FU (IC50 = 8.34 µM) in the C6 cancer cell line, and it had

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Hidayat, Ace Tatang, Kindi Farabi, Desi Harneti, et al. "A Cytotoxic Rocaglate Compound from The Stembark of Aglaia argentea (Meliaceae)." Molekul 12, no. 2 (2017): 146. http://dx.doi.org/10.20884/1.jm.2017.12.2.361.

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The Aglaia genus belong to Meliceae family is unique plant species because the presence of rocaglate and rocaglamide which is so far isolated only from Aglaia genus, indicate that type of this compound as a chemical marker for the genus of Aglaia. This type of compound known to have strong activity, such as insecticide and cytotoxic. This study describe the isolation, structure elucidation, and cytotoxic activity of an isolated rocaglate compound. Dried stembark of A. argentea extracted with methanol and partition between n-hexane, ethyl acetate, and n-butanol, respectively The extracts were t

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Bednarczyk-Cwynar, Barbara, Andrzej Günther, Piotr Ruszkowski, Szymon Sip, and Przemysław Zalewski. "Oleanolic Acid Lactones as Effective Agents in the Combat with Cancers—Cytotoxic and Antioxidant Activity, SAR Analysis, Molecular Docking and ADMETox Profile." International Journal of Molecular Sciences 26, no. 9 (2025): 4099. https://doi.org/10.3390/ijms26094099.

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Oleanolic acid derivatives, specifically lactones (2–8) and bromolactones (9–14), were synthesised and evaluated for their cytotoxic, antioxidant, and pharmacokinetic profiles. The compounds were characterised using molecular docking simulations targeting the 1M17 protein, representing the EGFR tyrosine kinase domain. Compound 6 emerged as the most promising candidate, demonstrating strong interactions with residues critical for EGFR activity, such as LYS 721 and ASP 831. Biological assays revealed that compounds 6, 2, and 10 exhibited IC50 values across various cancer cell lines in the microm

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El-Neketi, Mona, Weaam Ebrahim, Ngoc Tu Duong, et al. "Cytotoxic Rocaglamide Derivatives from Aglaia duppereana." Zeitschrift für Naturforschung C 68, no. 7-8 (2013): 269–74. http://dx.doi.org/10.1515/znc-2013-7-803.

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Phytochemical investigation of Aglaia duppereana flowers led to the isolation of a new rocaglamide derivative and twelve known congeners. The structure of the new compound was unambiguously elucidated by spectroscopic techniques (1D- and 2D-NMR, HRESIMS). The isolated compounds exhibited a potent cytotoxic activity against mouse lymphoma (L5178Y) cells with EC50 values ranging from 5.1 to 54.8 nM

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Fadayomi, Idowu E., Okiemute R. Johnson-Ajinwo, Elisabete Pires, et al. "Clerodane Diterpenoids from an Edible Plant Justicia insularis: Discovery, Cytotoxicity, and Apoptosis Induction in Human Ovarian Cancer Cells." Molecules 26, no. 19 (2021): 5933. http://dx.doi.org/10.3390/molecules26195933.

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Objectives: The toxicity of chemotherapeutic anticancer drugs is a serious issue in clinics. Drug discovery from edible and medicinal plants represents a promising approach towards finding safer anticancer therapeutics. Justicia insularis T. Anderson (Acanthaceae) is an edible and medicinal plant in Nigeria. This study aims to discover cytotoxic compounds from this rarely explored J. insularis and investigate their underlying mechanism of action. Methods: The cytotoxicity of the plant extract was evaluated in human ovarian cancer cell lines and normal human ovarian surface epithelia (HOE) cell

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Sayed, Mai M., Zohour I. Nabil, Nahla S. El-Shenawy, Rasha A. Al-Eisa, and Mohamed S. Nafie. "In Vitro and In Vivo Effects of Synthesis Novel Phenoxyacetamide Derivatives as Potent Apoptotic Inducer against HepG2 Cells through PARP-1 Inhibition." Pharmaceuticals 16, no. 11 (2023): 1524. http://dx.doi.org/10.3390/ph16111524.

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To discover potential cytotoxic agents, new semi-synthetic phenoxy acetamide derivatives, compound I and compound II, were synthesized, characterized, and screened for their cytotoxic activity against breast cancer (MCF-7) and liver cancer (HepG2) cell lines. The two compounds were more promising against HepG2 than the MCF-7 cell line according to IC50 values. When tested against the HepG2 cell line, compound I, and compound II both had significantly increased cytotoxic activity when compared to the reference medication 5-Fluorouracil (5-FU), with IC50 values of 1.43 M, 5.32 M, and 6.52 M for

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Ahanj, Negin, Mehdi Taghavi, and Ayyub Mojaddami. "Evaluation of Cytotoxicity and Molecular Docking Studies of Phthalimide and Naphthalimide Derivatives as Potential Anticancer Agents." Jundishapur Journal of Medical Sciences 20, no. 4 (2021): 366–75. http://dx.doi.org/10.32598/jsmj.20.4.2456.

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Background and Objectives Cancer is the second leading cause of death in the world after cardiovascular disease, so the aim of the present study was to investigate phthalimide and naphthalimide derivatives in order to develop anticancer compounds. Subjects and Methods In this study, the cytotoxic activity of six phthalimed and naphthalamide derivatives was evaluated using MTT method on three cancerous cell lines, including breast cancer (MCF-7), ovarian cancer (SKOV3) and lung cancer (A549) cell line. Molecular Docking studies were also performed to determine the binding energy and the compoun

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Hakimah, Wafiq Kholifatul, Ahmad Fauzi, Muhammad Reza Ramadhan, and Fariha Mufidah Maulina. "SYNTHESIS OF DIHYDROPYRIMIDINONE DERIVATIVES AND CYTOTOXIC ACTIVITY TEST AGAINST T47D CANCER CELLS." Medical Sains : Jurnal Ilmiah Kefarmasian 10, no. 2 (2025): 145–52. https://doi.org/10.37874/ms.v10i2.1693.

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Dihydropyrimidinone (DHPM) derivatives are heterocyclic compounds known for a variety of biological activities including anticancer properties. The Mitsunobu reaction was used in this study to synthesize a new DHPM derivative, ethyl 4-(4-isopropoxy-3,5-dimethylphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate (compound B2), and assess its cytotoxic activity against T47D breast cancer cells. Compound B2 was synthesized from ethyl 4-(4-hydroxy-3,5-dimethylphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate (compound M1) using multicomponent reactions (MCR) and the M

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Kilic-Kurt, Zühal, Filiz Bakar-Ates, Bahriye Karakas, and Özgür Kütük. "Cytotoxic and Apoptotic Effects of Novel Pyrrolo[2,3-d]Pyrimidine Derivatives Containing Urea Moieties on Cancer Cell Lines." Anti-Cancer Agents in Medicinal Chemistry 18, no. 9 (2019): 1303–12. http://dx.doi.org/10.2174/1871520618666180605082026.

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Background: Pyrrolo[2,3-d]pyrimidines have been recently reported to have anticancer activities through inhibition of different targets such as, Epidermal Growth Factor Receptor (EGFR) tyrosine kinase, Janus Kinase (JAK), mitotic checkpoint protein kinase (Mps1), carbonic anhydrase, MDM-2. On the other hand, aryl urea moieties which are found in some tyrosine kinase inhibitors such as Sorafenib and Linifanib have aroused recent attention as responsible for anticancer activities. The aims of this paper are to synthesize pyrrolo[ 2,3-d]pyrimidine derivatives containing urea moiety and evaluate t

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Ovando-Medina, Isidro, Leny P. Pérez-Díaz, Sonia Ruiz-González, Miguel Salvador-Figueroa, Marcos E. Urbina-Reyes, and Lourdes Adriano-Anaya. "Production of cytotoxic compounds in dedifferentiated cells ofJatropha curcasL. (Euphorbiaceae)." PeerJ 4 (November 1, 2016): e2616. http://dx.doi.org/10.7717/peerj.2616.

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This study addresses thein vitroculture as an alternative to obtain compounds with cytotoxic activity from the medicinal plantJatropha curcas(Euphorbiaceae). We determined the presence of cytotoxic compounds in both whole plants and dedifferentiated cells. We evaluated the effect of auxin, cytokinins and light on callus induction in cotyledon explants. We found that the most effective combination to induce callus was the auxin 2,4-D (5 mM) with the cytokinin 6-BAP (2.5 mM), on Murashige-Skoog medium in darkness. We compared the callogenic potential among accessions from different geographic or

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Jaidee, Atchara, Thanika Promchai, Kongkiat Trisuwan, et al. "Cytotoxic and Antimalarial Alkaloids from the Twigs of Dasymaschalon obtusipetalum." Natural Product Communications 10, no. 7 (2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000709.

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One new p-quinonoid aporphine alkaloid, obtusipetadione (1), and eleven known compounds (2–12) were isolated from the acetone extract of the twigs of Dasymaschalon obtusipetalum. Their structures were elucidated by spectroscopic methods. The cytotoxic and antimalarial activities of the isolated compounds were evaluated. Compound 1 showed significant in vitro antiplasmodial activity against the P. falciparum strains TM4 and K1 (multidrug resistant strain) with IC50 values of 2.46±0.12 and 1.38±0.99 μg/mL, respectively with no cytotoxicity. Compound 9 had more modest antiplasmodial activity, but

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