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

Simple item page
dc.contributor.authorIlhan S.
dc.contributor.authorÇamli Pulat Ç.
dc.contributor.authorOguz F.
dc.contributor.authorBektaş H.
dc.contributor.authorMenteşe E.
dc.contributor.authorAtmaca H.
dc.date.accessioned2024-07-22T08:02:32Z
dc.date.available2024-07-22T08:02:32Z
dc.date.issued2023
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 µg/mL. Among all derivatives, compounds C1 and D1 demonstrated a higher cytotoxic effect on cancer cells with IC50 values < 50 µg/mL, while a lower cytotoxic effect against human embryonic kidney cells with IC50 values of > 100 µg/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. Graphical abstract: [Figure not available: see fulltext.]. © 2022, The Author(s), under exclusive licence to Springer Nature Switzerland AG.
dc.identifier.DOI-ID10.1007/s11030-022-10524-3
dc.identifier.issn13811991
dc.identifier.urihttp://akademikarsiv.cbu.edu.tr:4000/handle/123456789/11885
dc.language.isoEnglish
dc.publisherInstitute for Ionics
dc.subjectAntineoplastic Agents
dc.subjectApoptosis
dc.subjectBenzimidazoles
dc.subjectCell Line, Tumor
dc.subjectCell Proliferation
dc.subjectHumans
dc.subject2 (5,6 dichloro 2 ethyl 1h benzimidazol 1 yl) n' [4 oxo 3 phenyl 1,3 thiazolidin 2 ylidene] acetohydrazide
dc.subject2 [(5,6 dichloro 2 ethyl 1h benzimidazol 1 yl) acetyl] n phenylhydrazine carboamide
dc.subject5 [(5,6 dichloro 2 ethyl 1h benzimidazol 1 yl) methyl] 4 phenyl 4h 1,2,4 triazol 3 ol
dc.subject5 [(5,6 dichloro 2 ethyl 1h benzimidazol 1 yl) methyl] n phenyl 1,3,4 thiadiazol 2 amine
dc.subject5 [(5,6 dichloro 2 ethyl 1h benzimidazol 1 yl)methyl] n phenyl 1,3,4 oxadiazol 2 amine
dc.subjectantineoplastic agent
dc.subjectbenzimidazole derivative
dc.subjectmessenger RNA
dc.subjectprotein bcl 2
dc.subjectunclassified drug
dc.subjectantineoplastic agent
dc.subjectbenzimidazole derivative
dc.subjectantineoplastic activity
dc.subjectapoptosis
dc.subjectArticle
dc.subjectclinical effectiveness
dc.subjectcontrolled study
dc.subjectcytotoxicity
dc.subjectdrug design
dc.subjectdrug effect
dc.subjectdrug efficacy
dc.subjectdrug mechanism
dc.subjectdrug response
dc.subjectdrug structure
dc.subjectdrug synthesis
dc.subjectH69AR cell line
dc.subjecthuman
dc.subjecthuman cell
dc.subjectIC50
dc.subjectMCF-7 cell line
dc.subjectMTT assay
dc.subjectPC3 cell line
dc.subjectprostate cancer cell line
dc.subjectprotein expression
dc.subjectprotein targeting
dc.subjectreal time polymerase chain reaction
dc.subjectT98G cell line
dc.subjectWestern blotting
dc.subjectapoptosis
dc.subjectcell proliferation
dc.subjecttumor cell line
dc.titleDesign and synthesis of benzimidazole derivatives as apoptosis-inducing agents by targeting Bcl-2 protein
dc.typeArticle

Files

Collections

Scopus Koleksiyonu