Azaindole structural framework is an integral part of several biologically active natural and synthetic organic molecules; and several FDA approved drugs for various diseases. In the last decade, quite a number of literature reports appeared describing the pharmacology, biological activity and therapeutic applications of a variety of azaindole molecules. This prompted the organic and medicinal chemistry community to develop novel synthetic methods for various azaindoles and test them for a bioactivity against a variety of biological targets. Herein, we have summarized the biological activity of therapeutically advanced clinical candidates and several preclinical candidate drugs that contain azaindole structural moiety.

氮杂吲哚结构框架是几种具有生物活性的天然和合成有机分子的组成部分；以及几种 FDA 批准的治疗各种疾病的药物。在过去的十年中，出现了相当多的文献报道，描述了各种氮杂吲哚分子的药理学、生物学活性和治疗应用。这促使有机和药物化学界为各种氮杂吲哚开发新的合成方法，并测试它们对各种生物靶标的生物活性。在此，我们总结了治疗先进的临床候选药物和几种含有氮杂吲哚结构部分的临床前候选药物的生物活性。