Abstract  Heterocyclic moiety serve as perfect framework on which pharmacophores can be effectively attached to produce novel drugs. Among various heterocyclic compounds,  nitrogen-based heterocycles have been extensively investigated as they constitute the core structures of numerous biologically relevant molecules and have been found to be active against different types of cancers. Due to the versatility of indole, it has been a highly “privileged motif” for the target-based design and development of anticancer agents. Moreover, it has been used as a synthon for the preparation of large number of bioactive heterocycles and paved a way to develop effective targets. This review article presents comprehensive overview of anticancer potentiality of diversely substituted indole derivatives including 1H-indole-2,3-dione and Spiro indole derivatives.