Cancer is one of the deadliest diseases in many developed and developing countries. Continuous efforts are required for designing better therapeutic agents for the treatment of cancer with more efficacy, selectivity, and less toxicity. The fused heterocyclic ring system has been identified by several researchers as a privileged structure that can be used as a basis for drug discovery in medicinal chemistry. The hetero-aromatic bicyclic ring system acts as a pharmacophore in a wide range of drugs with therapeutic potential. According to studies in the literature, variously substituted benzimidazoles have distinct pharmacological profiles with multi-targeting ability, making them an important anchor for the production of novel therapeutic agents against complex cancers including breast cancer, skin cancer, and blood cancer. In this presented article we are discussed various synthetic methods for the synthesis of anticancer benzimidazoles and their derivatives in different solvent conditions, substrates, and various catalysts mainly those which are eco-friendly, and economical, which shows the anticancer activity. We also focused on various derivatives are under clinical trials containing Benzimidazole moiety.
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