ReviewMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents2026
7-azaindole as privileged scaffold: Advances in drug design and structural modification.
Review in Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
7-azaindole is a nitrogen-containing heterocycle derived from indole, which has emerged as a privileged scaffold in drug design owing to its unique electronic distribution, spatial conformation, and dual-site hydrogen-bonding pharmacophore. Compared with indole, it exhibits enhanced hydrogen-bonding capacity, improved stability, and metabolic tolerance, while also allowing facile optimization of solubility, selectivity, and pharmacokinetic (PK) properties. Consequently, the 7-azaindole scaffold has been widely employed in the development of kinase inhibitors, anti-inflammatory agents, and neuro-modulatory agents. Approved drugs such as vemurafenib, pexidartinib, and venetoclax exemplify its successful translation from fragment to drug. This review comprehensively summarizes medicinal chemistry advances based on the 7-azaindole scaffold from 2020 to 2026, and critically consolidates SAR trends, pinpoints the most frequently successful substitution vectors, and dissects recent clinical failures. It aims to provide a reference for the future development of novel 7-azaindole-based therapeutics.
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