4.7 Review

Total synthesis, chemical modification and structure-activity relationship of bufadienolides

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 189, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112038

Keywords

Chan'Su; Bufadienolide; Cardiac steroids; Heart disease; Anti-Tumor

Funding

  1. National Natural Science Foundation of China [81973171]
  2. Priority Academic Program Development of Jiangsu Higher Education Institutions
  3. Flagship Major Development of Jiangsu Higher Education Institutions [PPZY2015A070]
  4. Key Laboratory of Therapeutic Material of Chinese Medicine, Jiangsu Province
  5. State Key Laboratory Cultivation Base for TCM Quality and Efficacy, Nanjing University of Chinese Medicine

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Bufadienolides are a type of natural cardiac steroids and originally isolated from the Traditional Chinese Medicine Chan'Su, they have been used for the treatment of heart disease in traditional remedies as well as in modern medicinal therapy with potent anti-tumor activities. Due to their unique molecular structures with unsaturated six-membered lactones attached to the steroid core, bufadienolides have received great attention in the synthetic organic community. This review presents total synthetic efforts to some representative bufadienolides, chemical modification of bufadienolides will also be given to discuss their structure-activity relationship in anti-tumor. (C) 2020 Elsevier Masson SAS. All rights reserved.

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