Triazolo‐linked benzimidazoles as tubulin polymerization inhibitors and DNA intercalators: Design, synthesis, cytotoxicity, and docking studies

摘要: A simple “click” protocol was employed in the quest of synthesizing 1,2,3‐triazole‐linked benzimidazoles as promising anticancer agents on various human cancer cell lines such as A549, HCT116, SK‐Mel‐28, HT‐29, and MCF‐7. Compound 12j demonstrated significant cytotoxic potential towards SK‐Mel‐28 cancer cells (IC50: 4.17 ± 0.09 µM) and displayed no cytotoxicity (IC50: > 100 µM) against normal human BEAS‐2B cells inferring its safety towards normal healthy cells. Further to comprehend the underlying apoptosis mechanisms, AO/EB, dichlorodihydrofluorescein diacetate (DCFDA), and 4',6‐diamidino‐2‐phenylindole (DAPI) staining were performed, which revealed the nuclear and morphological alterations. Compound 12j displayed impairment in cellular migration and inhibited colony formation. The annexin V binding assay and JC‐1 were implemented to evaluate the scope of apoptosis and …