This review presents 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 developed and developing
countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives
showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous
base i.e. purine. The review discussed benzimidazole derivatives showing anticancer
properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases,
DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism
and the substituents reported from the earlier and recent research articles are prerequisites for
the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses
on an easy comparison of the substituent essential for potency and selectivity through SAR presented
in figures. This will further provide a better outlook or fulfills the challenges faced in the
development of novel benzimidazole derivatives as anticancer.