ABSTRACT Indazole tautomers (1 H ‐ and 2 H ‐) have emerged as privileged scaffolds in drug discovery due to their unique hydrogen‐bonding properties, aromatic stability and ability to interact with many oncogenic targets. These structural characteristics of indazole derivatives make them a promising chemical moiety for the development of anticancer drugs. This review aims to elucidate the structural features of indazole derivatives that contribute to their anticancer potential while summarising recent advances in their biological evaluation. Recent studies have revealed that an indazole derivative exhibits several anticancer activities, including kinase inhibition, cell‐cycle arrest, apoptosis, DNA interactions and modulation of critical oncogenic pathways. Computational studies supporting structural validation were also discussed to correlate the substitution pattern with biological potency. Discussed patents may highlight innovative synthetic strategies and hybrid molecular designs. In this review, the most active indazole‐based compounds are discussed, along with their IC 50 values, key structural features and supporting biological evaluations (cell line studies, molecular targets: AURKs, CDKs, EGFR, FGFR, HIF‐1, ER‐α, MAPKs, PDKs and in vivo studies). Indazole derivatives with potent activity exhibit nano‐ to micromolar IC 50 values, with strategic substitutions markedly improving efficacy and selectivity, highlighting indazole as a potential anticancer scaffold.
Vajidwal et al. (Mon,) studied this question.