Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship

• Published in: European journal of medicinal chemistry Vol. 223; p. 113652
• Main Authors: Wang, Hezhen, Wang, Zhiyuan, Wei, Chunyong, Wang, Jing, Xu, Yingshu, Bai, Guohui, Yao, Qizheng, Zhang, Lei, Chen, Yongzheng
• Format: Journal Article
• Language: English
• Published: Elsevier Masson SAS 05.11.2021
• Subjects: Anticancer activity; Bisindole alkaloid; Indirubin; Mechanism; Structural modification; Structure-activity relationship; Structural modification; Indirubin; Structure-activity relationship; Mechanism; Anticancer activity; Bisindole alkaloid
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2021.113652

Indirubin is the crucial ingredient of Danggui Longhui Wan and Qing-Dai, traditional Chinese medicine herbal formulas used for the therapy of chronic myelocytic leukemia in China for hundreds of years. Although the monomeric indirubin has been used in China for the treatment human chronic myelocytic leukemia. However, due to low water solubility, poor pharmacokinetic properties and low therapeutic effects are the major obstacle, and had significantly limited its clinical application. Consequently, the attractive anticancer profile of indirubin has enthused numerous researchers to discover novel indirubin derivatives with improved pharmacodynamic activity as well as good pharmacokinetic property. In this paper, we comprehensively review the recent progress of anticancer potential of indirubins, structural modification and structure-activity relationship, which may provide useful direction for the further development of novel indirubins with improved pharmacological profiles for the treatment of various types of cancer. This review covers the recent advances of anticancer potential of indirubins, structural modification and structure-activity relationship, which may provide useful direction for the further development of novel indirubins with improved pharmacological profiles. [Display omitted] •Indirubin is an important natural bisindole alkaloid for anticancer drug exploration.•The recent advances of structural modification of indirubin were comprehensively summarized.•The multiple mechanisms underlying the anticancer action were included.•The structure-activity relationship was discussed.•The review will be conducive to the medicinal research of indirubin.