Synthetic strategies and therapeutic insights into FDA-approved indole-containing drugs
Tengjiao Yang, Yanfeng Zhang, Peng Liu, Peng Qi, Xiankai Li, Wubin Zhi, Lijie Zhao
TL;DR
This review explores FDA-approved drugs containing indole, highlighting their synthetic methods and therapeutic uses to guide future drug development.
Contribution
The paper offers a comprehensive survey of recent FDA-approved indole-based drugs and their synthetic strategies.
Findings
Indole-based drugs are used in oncology, infectious diseases, and other therapeutic areas.
Synthetic strategies highlight the versatility of the indole scaffold in drug design.
The review integrates chemistry and clinical data to guide future drug development.
Abstract
Indole is a privileged heteroaromatic scaffold in medicinal chemistry, characterised by its unique physicochemical properties, hydrogen-bonding potential, and bioisosteric versatility. Over the past decades, numerous indole-containing drugs have been approved by the Food and Drug Administration (FDA), spanning diverse therapeutic areas including oncology, infectious diseases, gastrointestinal disorders, neurological conditions, and cardiovascular diseases. This review provides a comprehensive survey of FDA-approved indole-based drugs, with particular emphasis on those approved from 2013 to the present. Representative synthetic strategies are highlighted to illustrate the versatility of the indole framework in drug design. Furthermore, we systematically discuss each drug’s pharmacology, mechanisms of action, and clinical applications. By integrating synthetic chemistry with clinical…
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Taxonomy
TopicsSynthesis of Indole Derivatives · Catalytic C–H Functionalization Methods · Click Chemistry and Applications