Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy

Yanghan Liu, Yongqiang Liu, Zhen Li, Guang Biao Zhou, Zhu Jun Yao, Sheng Jiang

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

A series of novel bivalent mimetics of annonaceous acetogenins have been designed, synthesized, and evaluated. Among these, compound 7 bearing a homopiperazine ring in the middle region exhibited more potent growth inhibitory activity and higher selectivity against cancer cells over normal cells by comparison with AA005. This work indicates that modification of the middle piperazine ring is a useful optimizing tool for the simplified acetogenin mimetics.

Original languageEnglish (US)
Pages (from-to)1650-1653
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number7
DOIs
StatePublished - Apr 1 2014

Keywords

  • Annonaceous acetogenins
  • Bivalent analogues
  • Cytotoxicity
  • Homopiperazine
  • Selectivity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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