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Background: Cancer is a life-threatening disease. Anti-cancer drugs are the focus of research. The heterocyclic molecules like benzimidazole occupy a central position in searching for novel and effective anti-cancer drugs. The medicinal chemists designed and synthesized several benzimidazole derivatives and conjugates to evaluate them as potential anti-cancer agents. Objective: The purpose of this compilation of literature is to cover the progress of benzimidazole-based anti-cancer agents, their synthesis, and their evaluation for cancer disease treatment. Methods: The recent literatures have been collected from various search engines and peer-reviewed journals. Results: The compounds like benzimidazole derivatives of dehydroabietic acid, piperidyl benzimidazole carboxamide, benzimidazole-quinazolinone hybrids, benzimidazole-thiazole conjugate, and benzimidazole pendant cyanopyrimidine derivatives have been discussed in detail. Conclusion: This review article will help the medicinal chemists to design and synthesize benzimidazole-based molecules and evaluate them as anti-cancer agents.