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

被引：49

作者：

Wang, Hezhen ^{[1
]}

Wang, Zhiyuan ^{[1
]}

Wei, Chunyong ^{[1
]}

Wang, Jing ^{[1
]}

Xu, Yingshu ^{[1
]}

Bai, Guohui ^{[2
]}

Yao, Qizheng ^{[3
]}

Zhang, Lei ^{[1
]}

Chen, Yongzheng ^{[1
]}

机构：

[1] Zunyi Med Univ, Sch Pharm, Key Lab Biocatalysis & Chiral Drug Synth Guizhou, Key Lab Basic Pharmacol,Minist Educ, 6 West Xuefu Rd, Zunyi 563000, Guizhou, Peoples R China

[2] Zunyi Med Univ, Key Lab Oral Dis Higher Sch Guizhou Prov, 6 West Xuefu Rd, Zunyi 563000, Guizhou, Peoples R China

[3] China Pharmaceut Univ, Sch Pharm, 24 Tongjia Xiang, Nanjing 210009, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2021年 / 223卷

基金：

中国国家自然科学基金;

关键词：

Indirubin; Bisindole alkaloid; Anticancer activity; Structural modification; Mechanism; Structure-activity relationship; CHINESE ANTILEUKEMIA MEDICINE; CHRONIC MYELOGENOUS LEUKEMIA; CELL-CYCLE ARREST; GLYCOGEN-SYNTHASE KINASE-3; PROSTATE-CANCER CELLS; IN-VITRO; INDIGO-NATURALIS; ANTIPROLIFERATIVE ACTIVITY; ANTITUMOR-ACTIVITY; PANCREATIC-CANCER;

D O I：

10.1016/j.ejmech.2021.113652

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

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