Vol. 7, Issue 2, Part B (2025)

Cancer continues to be a leading global health burden, prompting the need for innovative therapeutic strategies that address treatment resistance, toxicity, and specificity. Benzimidazole and its derivatives have emerged as promising pharmacophores in oncology due to their versatile biological activities, including kinase inhibition, microtubule disruption, and modulation of apoptosis pathways. This review explores recent advances in the development of benzimidazole-based compounds targeting various cancers, such as glioblastoma, colorectal cancer, leukaemia, breast, and lung malignancies. Notable examples include inhibitors of the neddylation pathway, tubulin-binding agents, and kinase-targeting molecules, which demonstrate potent in vitro and in vivo efficacy. Several benzimidazole derivatives, such as compound 12b and 7c, exhibited low nanomolar cytotoxicity and overcame drug resistance mechanisms, particularly in paclitaxel- and EGFR-TKI-resistant models. Additionally, benzimidazole–triazole hybrids have shown dual functionality by serving as both cytotoxic agents and PET imaging probes through Galectin-1 targeting. The integration of computational modelling, cell line assays, molecular docking, and clinical trials underlines the translational relevance of these scaffolds. Collectively, benzimidazoles represent a promising platform for developing next-generation anticancer therapeutics and diagnostic agents, particularly in the context of precision medicine.