Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison
Copyright policy )Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison
In this study, some benzimidazole-oxadiazole derivatives were synthesised and tested for their in vitro anticancer activities on five cancer cell lines, including HeLa, MCF7, A549, HepG2 and C6. Their structures were elucidated by IR, 1H-NMR, 13C-NMR, 2 D-NMR and HRMS spectroscopic methods. Among all screened compounds; 5a, 5b, 5d, 5e, 5k, 5l, 5n and 5o exhibited potent selective cytotoxic activities against various tested cancer cell lines. Especially, compounds 5l and 5n exhibited the most antiproliferative activity than Hoechst 33342 and doxorubicin against HeLa cell line, with IC50 of 0.224 ± 0.011 µM and 0.205 ± 0.010 µM, respectively. Furthermore, these potent lead cytotoxic agents were evaluated in terms of their inhibition potency against Topoisomerase I and it was determined that selected compounds inhibited the Topoisomerase I. Docking studies were performed and probable interactions in the DNA-Topo I enzyme complex was determined.
- Anadolu University Turkey
- ZONGULDAK BULENT ECEVIT UNIVERSITY Turkey
- Bülent Ecevit University Turkey
Antineoplastic Agents, RM1-950, anticancer, benzimidazole, Cell Line, Mice, Structure-Activity Relationship, 1,3,4-oxadiazole, Animals, Humans, dna topo i, 0104 chemical sciences, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, 01 natural sciences, hoechst 33342, 3. Good health, Molecular Docking Simulation, DNA Topoisomerases, Type I, Therapeutics. Pharmacology, Drug Screening Assays, Antitumor, Topoisomerase I Inhibitors, Research Paper
Antineoplastic Agents, RM1-950, anticancer, benzimidazole, Cell Line, Mice, Structure-Activity Relationship, 1,3,4-oxadiazole, Animals, Humans, dna topo i, 0104 chemical sciences, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, 01 natural sciences, hoechst 33342, 3. Good health, Molecular Docking Simulation, DNA Topoisomerases, Type I, Therapeutics. Pharmacology, Drug Screening Assays, Antitumor, Topoisomerase I Inhibitors, Research Paper
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).43 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!