Biological evaluation of new mimetics of annonaceous acetogenins: Alteration of right scaffold by click linkage with aromatic functionalities

Yanghan Liu, Qicai Xiao, Yongqiang Liu, Zheng Li, Yatao Qiu, Guang Biao Zhou, Zhu Jun Yao, Sheng Jiang

Research output: Contribution to journalArticle

9 Scopus citations

Abstract

A small library of analogues of annonaceous acetogenins through click linkage with aromatic moieties is established using a convergent modular fragment-assembly approach. These analogues exhibited low micromolar inhibitory activities against the proliferation of several human cancer cell lines. Structure-activity relationship (SAR) of these analogues indicates that replacement of the methoxy groups of ubiquinone ring with methyl groups is proved to be a useful strategy for improving the anticancer activity of quinone-acetogenin hybrids.

Original languageEnglish (US)
Pages (from-to)248-258
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume78
DOIs
StatePublished - May 6 2014

Keywords

  • Annonaceous acetogenins
  • Aromatic functionalities
  • Click chemistry
  • Cytotoxicity
  • Quinone

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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