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: This review presented the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical society has shown progressive development in fighting cancer. Researchers all over the world in both the developed and developing countries are in continous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with natuarally occurring nitrogenous base i.e purine. The review discussed about benzimidazole derivatives showing anticancer properties through different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes and tubulin inhibitors. Benzimidazole derivatives act through different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.

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Depression is the single largest contributor to global disability with a huge economic and social burden on the world. There are a number of antidepressant drugs on the market, but treatment‐resistant depression and relapse of depression in a large number of patients have increased problems for clinicians. One peculiarity observed in most of the marketed antidepressants is the presence of a piperazine substructure. Although piperazine is also used in the optimization of other pharmacological agents, it is almost extensively used for the development of novel antidepressants. One common understanding is that this is due to its favorable CNS pharmacokinetic profile; however, in the case of antidepressants, piperazine plays a much bigger role and is involved in specific binding conformations of these agents. Therefore, in this review, a critical analysis of the significance of the piperazine moiety in the development of antidepressants has been performed. An overview of current developments in the designing and synthesis of piperazine‐based antidepressants (2015 onwards) along with SAR studies is also provided. The various piperazine‐based therapeutic agents in early‐ or late‐phase human testing for depression are also discussed. The preclinical compounds discussed in this review will help researchers understand how piperazine actually influences the design and development of novel antidepressant compounds. The SAR studies discussed will provide crucial clues about the structural features and optimizations required to enhance the efficacy and potency of piperazine‐based antidepressants.

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