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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 223, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113652

Keywords

Indirubin; Bisindole alkaloid; Anticancer activity; Structural modification; Mechanism; Structure-activity relationship

Funding

  1. National Natural Science Foundation of China, China [81860622]
  2. Joint Fund of the Department of Science and Technology of Zunyi City and Stomatological Hospital of Zunyi Medical University, China [[2020]293]
  3. Joint Fund of the Department of Science and Technology of Zunyi City and Zunyi Medical University, China [[2018]27]
  4. Priming Scientific Research Foundation for Master Program of Zunyi Medical University, China [F-963]
  5. Education and Teaching Reform Program of Zunyi Medical University, China [ZYK38]
  6. Construction Projects of Medical Biomaterial Research & Development Talent Base in Guizhou Province and Zunyi City, China [[2018]3, [2019] 69]
  7. Science and Technology Department of Zunyi, China [ZSKRPT2020-5]

Ask authors/readers for more resources

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.
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.

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