4.4 Review

Indazole as a Privileged Scaffold: The Derivatives and their Therapeutic Applications

期刊

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
卷 21, 期 7, 页码 839-860

出版社

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520620999200818160350

关键词

Heterocyclic compound; indazole; therapeutic application; structure-activity relationship; pharmacology; activity

资金

  1. National Natural Science Foundation of China [81903623]
  2. China Postdoctoral Science Foundation [2019M652586]
  3. Postdoctoral Research Grant in Henan Province [19030008]

向作者/读者索取更多资源

This study provides an overview of the mechanism and structure-activity relationship of indazole and its derivatives, categorizing them into six groups based on their versatile biological activities. At least 43 indazole-based therapeutic agents are currently in clinical use or clinical trials. Future research directions include exploring more diverse bioactive moieties with indazole scaffold and gaining greater insights into its mechanism.
Background: Heterocyclic compounds, also called heterocycles, are a major class of organic chemical compound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. Methods: A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. Results: The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. Conclusion: This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compounds where the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.

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