In the current era, numerous anticancer drugs are available with potential
pharmacological activity. Still, issues like multi-drug resistance, toxicity, solubility
etc., were in existence, which finally decreases the overall therapeutic value of indices
of the drug molecule. Therefore, in search of new anticancer agents to fight against
cancer is not an ending process. Keeping this in view, aromatic diazole heterocyclic
nucleus named imidazole was proved with quite promising health benefits. The
imidazole nucleus possesses numerous pharmacological activities. Thus, its
derivatives/analogs have occupied a distinctive position in medicinal chemistry due to
the incorporation of the heterocyclic nucleus, imidazole, to develop the new synthetic
strategy in the significant drug discovery process. In addition to this, the significant
therapeutic potential of the imidazole containing agents have triggered the medicinal
chemist to develop a large number of novel anticancer compounds with a low toxicity
profile. This chapter aims ornately pronounced the therapeutic voyage of imidazole and
its analogs as anticancer.
Keywords: Anticancer, Benzimidazole, Cancer, Drug discovery, Imidazole.
