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Benzimidazole, the benzo derivative of imidazole, is a class of bicyclic aromatic organic compound consisting of six‐membered benzene ring fused to five‐membered imidazole at 4‐ and 5‐positions of the imidazole ring. It is a vital pharmacophore of many biologically active heterocyclic compounds with a variety of pharmacological activities. Over the time, benzimidazole and its derivatives have evolved as vibrant heterocyclic systems due to their potency in a wide range of bioactive compounds like analgesics, antifungals, anti‐inflammatory, antihypertensives, proton pump inhibitors, anti‐HIV, antiviral, and so on. Multi‐drug resistance in cancer that led to the failure of many chemotherapeutic drugs is a major concern. Various approaches are being developed to overcome this problem. One of them is target based drug discovery, which is an effective method to develop a novel anticancer drug. To develop newer drugs, previously reported work needs to be studied. Keeping this in mind, last 5 years literature on benzimidazole used as anticancer agents has been reviewed and summarized in the paper herein. This review article along with the target of cancer also deal with structure activity relationship of various compounds having benzimidazole ring. [ABSTRACT FROM AUTHOR]