Indole is a prestigious heterocyclic skeleton widely found in both naturally-occurring and biologically active compounds. Pharmaceutical agents containing indole skeleton in their frameworks always possess a wide range of pharmacological properties including antiviral, antitumor, analgesic and other therapeutic activities and many indole-containing drugs have been proved to have better pharmacokinetic and pharmacological effects. Over the past few decades, the FDA has approved over 40 indole-containing drugs for treating various clinical conditions and the development of indole-related drugs has gained 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.
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