Novel spirobicyclic artemisinin analogues (artemalogues): Synthesis and antitumor activities

Gang Liu, Shanshan Song, Shiqi Shu, Zehong Miao, Ao Zhang, Chunyong Ding

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

The sesquiterpene lactone framework of artemisinin was used as a drug repositioning prototype for the development of novel antitumor drugs. Several series of novel artemisinin analogues (artemalogues) were designed and synthesized through 1,3-dipolar cycloaddition of artemisitene with nitrile oxides or nitrones. The isoxazolidine-containing spirobicyclic artemalogue 11b turns out to be the most potent with low micromolar IC50 values against all three tumor cells, which were at least 4-to 14-fold more potent than the parent artemisinin.

Original languageEnglish (US)
Pages (from-to)17-28
Number of pages12
JournalEuropean Journal of Medicinal Chemistry
Volume103
DOIs
StatePublished - Oct 20 2015
Externally publishedYes

Keywords

  • 1 3-dipolar cycloaddition
  • Antiprolifereative effect
  • Artemisinin
  • Spirobicyclic artemalogues
  • Stereoconfiguration

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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