Microtubules, as dynamic regulators in many cellular processes, remain pivotal targets in cancer chemotherapy. Among the structural motifs explored, the benzimidazole scaffold has emerged as a privileged heterocyclic ring system in the development of potent therapeutic agents, owing to its versatility and pharmacological relevance. This review critically examines the synthesis, anticancer activity, structure-activity relationships (SAR), and tubulin polymerization inhibitory properties of diverse benzimidazole derivatives. In addition, various synthetic strategies and innovative approaches for generating benzimidazole based analogs with enhanced cytotoxic profiles are highlighted. Recent findings underscore the potential of benzimidazole derivatives as promising tubulin polymerization inhibitors, contributing significantly to the discovery of next-generation anticancer agents.