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New series of benzimidazole‐1,2,4‐triazole derivatives were designed, synthesized, and characterized using 1H‐NMR, 13C‐NMR, and HRMS. These compounds were evaluated for anticancer activity toward HTB‐9 bladder and HT‐29 colorectal cancer cell lines. Compounds 7h and 7ı were found to be the most active against HTB‐9 cell line, with IC50 6.27 and 6.44 μM, respectively, comparable to positive control cisplatin (IC50 = 11.40 μM). Additionally, in HT‐29 cell line, compounds 7a and 7ı exhibited the lowest IC50 values (20.37 and 22.71 μM, respectively), which was higher than those of cisplatin (19.79 μM). All active compounds induced apoptosis and caspase 3/7 activity and reduced the migration ability in both cell lines. Particularly, HT‐29 cells treated with compound 7ı exerted a higher apoptotic index than cisplatin‐treated cells. Furthermore, compounds 7h and 7ı led to G1 cell cycle arrest of HTB‐9, and compounds 7a and 7ı against HT‐29 induced S and G1 cell cycle arrest, respectively. In conclusion, the antiproliferative effect of active compounds is associated with the induction of apoptosis through caspase 3/7 activation and cell cycle arrest at different phases in HTB‐9 and HT‐29 cell lines. [ABSTRACT FROM AUTHOR]

Cancer is the second leading cause of death today and remains a threat to human health. The advent of multi‐drug resistance and adverse effects make the current first‐line anti‐cancer medicines inadequate, despite the fact that numerous efforts have been made in the field of cancer therapy and significant progress has been made in the diagnosis and treatment of cancer. Consequently, the development of novel anticancer drugs with high activity and minimal toxicity is imperative. The benzimidazole ring has attracted the attention of medicinal chemists due to its medicinal and pharmacological properties. The heterocyclic pharmacophore of benzimidazole is a crucial scaffold for developing pharmaceuticals and drugs. In this review, we summarized the recent progress of benzimidazole as a privileged scaffold for the discovery of anti‐cancer agents based on biological targets, such as VEGFR (Vascular Endothelial Growth Factor), PI3 K inhibitors (Phosphoinositide 3‐kinase), EGFR kinase inhibitors (Epidermal Growth Factor Receptor), PARPs (Poly ADP‐ribose polymerases), Tubulin Polymerization, HAT/HDAC (histone acetylase/histone deacetylase), SphK1 (Sphingosine kinase‐1 inhibitors), aromatase, carbonic anhydrase, and topoisomerase inhibitors. The last 5 years of literature have been reviewed and relevant studies have been summarized in this review. [ABSTRACT FROM AUTHOR]