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

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. (C) 2021 Elsevier Masson SAS. All rights reserved.

Automated summary

Indirubin is a crucial ingredient in Chinese traditional medicine for treating leukemia. Despite its attractive anticancer profile, limitations like low water solubility and poor pharmacokinetic properties have hindered its clinical application. Researchers are exploring novel derivatives of indirubin with improved pharmacological profiles for cancer treatment.