Benzimidazole derivatives have attracted considerable attention in anticancer drug development owing to their structural mimicry of nucleosides, which enables disruption of key biological pathways involved in tumor growth and progression. Their ability to serve as both hydrogen bond donors and acceptors enhances binding to a variety of cancer-related molecular targets, contributing to their versatility and effectiveness. The adaptability of benzimidazole scaffolds permits optimal interaction with biopolymers, positioning them as promising nucleotide isosteres in medicinal chemistry. As a result, benzimidazole-based compounds continue to be recognized as vital heterocyclic pharmacophores, highlighting their significant potential for advancing novel anticancer therapies. The in-vitro activities of the benzimidazole derivatives showed good efficacy in preclinical studies and have potential for pharmacokinetic and safety profiles. This review highlights the synthesis of benzimidazole derivatives, its applications for different types of cancers. Further, anticancer mechanism with benzimidazole derivatives and their molecular docking studies is also discussed.
Panda et al. (2026) studied this question.