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<p>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.</p><p></p>

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7-azaindole as privileged scaffold: Advances in drug design and structural modification

  • 期刊论文

  • 发表日期：

    2026年7月23日

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  • Yichun Shi,
  • Guangjun Yu,
  • Yidan Xu,
  • Xindan Liao

摘要

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.