dc.contributor.author | İlhan, Süleyman | |
dc.contributor.author | Çamlı Pulat, Çisil | |
dc.contributor.author | Oğuz, Ferdi | |
dc.contributor.author | Bektaş, Hakan | |
dc.contributor.author | Menteşe, Emre | |
dc.contributor.author | Atmaca, Harika | |
dc.date.accessioned | 2022-11-21T08:20:30Z | |
dc.date.available | 2022-11-21T08:20:30Z | |
dc.date.issued | 2022 | en_US |
dc.identifier.citation | Ilhan, S., Çamli Pulat, Ç., Oguz, F., Bektaş, H., Menteşe, E., & Atmaca, H. (2022). Design and synthesis of benzimidazole derivatives as apoptosis-inducing agents by targeting Bcl-2 protein. Molecular diversity, https://doi.org/10.1007/s11030-022-10524-3 | en_US |
dc.identifier.issn | 1573-501X | |
dc.identifier.uri | https://doi.org/10.1007/s11030-022-10524-3 | |
dc.identifier.uri | https://hdl.handle.net/11436/7092 | |
dc.description.abstract | Bcl-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] | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Springer | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Benzimidazole derivatives | en_US |
dc.subject | Anticancer drugs | en_US |
dc.subject | Apoptosis | en_US |
dc.subject | Bcl-2 | en_US |
dc.title | Design and synthesis of benzimidazole derivatives as apoptosis-inducing agents by targeting Bcl-2 protein | en_US |
dc.type | article | en_US |
dc.contributor.department | RTEÜ, Fen - Edebiyat Fakültesi, Kimya Bölümü | en_US |
dc.contributor.institutionauthor | Menteşe, Emreq | |
dc.identifier.doi | 10.1007/s11030-022-10524-3 | en_US |
dc.relation.journal | Molecular Diversity | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |