Zeng Wei, Han Chi, Mohammed Sarah, Li Shanshan, Song Yixuan, Sun Fengxia, Du Yunfei
School of Pharmaceutical Science and Technology, Tianjin University Tianjin 300072 China
Department of Chemical Engineering & Biotechnology, University of Cambridge CB2 3RA Cambridge UK.
RSC Med Chem. 2024 Jan 30;15(3):788-808. doi: 10.1039/d3md00677h. eCollection 2024 Mar 20.
Indole is a prestigious heterocyclic skeleton widely found in both naturally-occurring and biologically-active compounds. Pharmaceutical agents containing an indole skeleton in their framework possess a wide range of pharmacological properties, including antiviral, antitumor, analgesic, and other therapeutic activities, and many indole-containing drugs have been proven to have excellent pharmacokinetic and pharmacological effects. Over the past few decades, the FDA has approved over 40 indole-containing drugs for the treatment of various clinical conditions, and the development of indole-related drugs has attracted significant attention from medicinal chemists. This review aims to provide an overview of all the approved drugs that contain an indole nucleus, focusing on their targets, pharmacological activities, and SAR studies.
吲哚是一种著名的杂环骨架，广泛存在于天然产物和生物活性化合物中。在其结构框架中含有吲哚骨架的药物制剂具有广泛的药理特性，包括抗病毒、抗肿瘤、镇痛及其他治疗活性，并且许多含吲哚的药物已被证明具有优异的药代动力学和药理作用。在过去几十年中，美国食品药品监督管理局（FDA）已批准40多种含吲哚的药物用于治疗各种临床病症，吲哚相关药物的开发已引起药物化学家的极大关注。本综述旨在概述所有已批准的含吲哚核的药物，重点关注其靶点、药理活性和构效关系研究。
