Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies

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dc.contributor.authorAtmaca H.
dc.contributor.authorİlhan S.
dc.contributor.authorBatır M.B.
dc.contributor.authorPulat Ç.Ç.
dc.contributor.authorGüner A.
dc.contributor.authorBektaş H.
dc.date.accessioned2024-07-22T08:07:20Z
dc.date.available2024-07-22T08:07:20Z
dc.date.issued2020
dc.description.abstractThe 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. Muse™ 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 μg/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 μg/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. © 2020 Elsevier B.V.
dc.identifier.DOI-ID10.1016/j.cbi.2020.109163
dc.identifier.issn00092797
dc.identifier.urihttp://akademikarsiv.cbu.edu.tr:4000/handle/123456789/13928
dc.language.isoEnglish
dc.publisherElsevier Ireland Ltd
dc.subjectAntineoplastic Agents
dc.subjectApoptosis
dc.subjectBenzimidazoles
dc.subjectCell Line, Tumor
dc.subjectDrug Screening Assays, Antitumor
dc.subjectG2 Phase Cell Cycle Checkpoints
dc.subjectHumans
dc.subject2 [5,6 dichloro 2 ethyl 1h benzimidazol 1 yl] n'[4 bromophenylene]acetohydrazide
dc.subject2 [5,6 dichloro 2 ethyl 1h benzimidazol 1 yl]acetohydrazide
dc.subject2 [[5,6 dichloro 2 ethyl 1h benzimidazol 1 yl]acetyl] n phenylhydrazine carbothioamide
dc.subject5 [[5,6 dichloro 2 ethyl 1h benzimidazol 1 yl]methyl] 4 phenyl 4h 1,2,4 triazole 3 thiol
dc.subjectantineoplastic agent
dc.subjectbenzimidazole derivative
dc.subjectethyl[5,6 dichloro 2 ethyl 1h benzimidazol 1 yl]acetate
dc.subjectfluorouracil
dc.subjectprotein p53
dc.subjectunclassified drug
dc.subjectantineoplastic agent
dc.subjectbenzimidazole derivative
dc.subjectapoptosis
dc.subjectArticle
dc.subjectcell cycle
dc.subjectcell cycle progression
dc.subjectcell population
dc.subjectcontrolled study
dc.subjectdrug cytotoxicity
dc.subjectdrug structure
dc.subjectdrug synthesis
dc.subjectDU145 cell line
dc.subjectG2 phase cell cycle checkpoint
dc.subjectH69AR cell line
dc.subjectHEK293 cell line
dc.subjecthuman
dc.subjecthuman cell
dc.subjectIC50
dc.subjectin vitro study
dc.subjectMCF-7 cell line
dc.subjectMTT assay
dc.subjectapoptosis
dc.subjectdrug effect
dc.subjectdrug screening
dc.subjectsynthesis
dc.subjecttumor cell line
dc.titleNovel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies
dc.typeArticle

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