Design and synthesis of benzimidazole derivatives as apoptosis-inducing agents by targeting Bcl-2 protein

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dc.contributor.authorIlhan, S
dc.contributor.authorPulat, ÇÇ
dc.contributor.authorOguz, F
dc.contributor.authorBektas, H
dc.contributor.authorMentese, E
dc.contributor.authorAtmaca, H
dc.date.accessioned2025-04-10T10:35:04Z
dc.date.available2025-04-10T10:35:04Z
dc.description.abstractBcl-2, an anti-apoptotic protein, is a well-known and appealing cancer therapy target. Novel series of benzimidazole derivatives were synthesized and tested for their activity as Bcl-2 inhibitors on T98G glioblastoma, PC3 prostate, MCF-7 breast, and H69AR lung cancer cells. MTT assay was used to evaluate the cytotoxic effect. PI Annexin V Apoptosis Detection Kit was used to detect apoptosis. Expression levels of the Bcl-2 protein were examined by the Western blot analysis and qRT-PCR. All synthesized benzimidazole derivatives exhibited a cytotoxic effect on cancer cells with IC50 values in the range of 25.2-88.2 mu g/mL. Among all derivatives, compounds C1 and D1 demonstrated a higher cytotoxic effect on cancer cells with IC50 values < 50 mu g/mL, while a lower cytotoxic effect against human embryonic kidney cells with IC50 values of > 100 mu g/mL. C1 and D1 caused a significant increase in the percentage of apoptotic cells in all types of cancer cell cells and both Bcl-2 mRNA and protein levels were significantly reduced. These results suggest that the novel benzimidazole derivatives may be candidates for apoptosis-inducing agents in cancer treatment by targeting anti-Bcl-2 proteins in cancer cells. [GRAPHICS]
dc.identifier.e-issn1573-501X
dc.identifier.issn1381-1991
dc.identifier.urihttp://hdl.handle.net/20.500.14701/41156
dc.language.isoEnglish
dc.titleDesign and synthesis of benzimidazole derivatives as apoptosis-inducing agents by targeting Bcl-2 protein
dc.typeArticle

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