Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies
| dc.contributor.author | Atmaca, H | |
| dc.contributor.author | Ilhan, S | |
| dc.contributor.author | Batir, MB | |
| dc.contributor.author | Pulat, CC | |
| dc.contributor.author | Güner, A | |
| dc.contributor.author | Bektas, H | |
| dc.date.accessioned | 2025-04-10T10:33:39Z | |
| dc.date.available | 2025-04-10T10:33:39Z | |
| dc.description.abstract | The aim of the study was to synthesize a new series of benzimidazole derivatives and to investigate the underlying molecular mechanisms of the potential cell cycle inhibition and apoptotic effects against a panel of selected human cancer cell lines along with HEK-293 human embryonic kidney cells. MTT assay was used to evaluate cytotoxic effects. MuseT Cell Analyzer was used to assess cell cycle progression. Annexin-V/PI staining assay was used for detecting apoptosis. All the synthesized compounds showed a significant cytotoxic effect against cancer cells with the IC50 values between 9.2 and 166.1 mu g/mL. Among the tested derivatives, compound 5 showed significant cytotoxic activity against MCF-7, DU-145 and H69AR cancer cells with the IC50 values of 17.8 +/- 0.24, 10.2 +/- 1.4 and 49.9 +/- 0.22 mu g/mL respectively. The compounds 5 was also tested on HEK-293 human embryonic kidney cells and found to be safer with lesser cytotoxicity. The results revealed that compound 5 significantly increased cell population in the G2/M-phase which is modulated by a p53 independent mechanism. Compound 5 caused an increase in the percentage of late apoptotic cells in all tested cancer cells in a concentration-dependent manner. Among all synthesized derivatives, compound 5 the bromo-derivative, showed the highest cytotoxic potential, induced G2/M cell cycle arrest and apoptotic cell death in genotypically different human cancer cells. These results suggest that compound 5 might be a promising agent for cancer therapy and further structural modifications of benzimidazole derivatives may create promising anticancer agents. | |
| dc.identifier.e-issn | 1872-7786 | |
| dc.identifier.issn | 0009-2797 | |
| dc.identifier.uri | http://hdl.handle.net/20.500.14701/39899 | |
| dc.language.iso | English | |
| dc.title | Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies | |
| dc.type | Article |