Potent antitumor mimetics of annonaceous acetogenins embedded with an aromatic moiety in the left hydrocarbon chain part

Qicai Xiao, Yongqiang Liu, Yatao Qiu, Guangbiao Zhou, Chan Mao, Zheng Li, Zhu Jun Yao, Sheng Jiang

Research output: Contribution to journalArticle

17 Scopus citations

Abstract

Annonaceous acetogenins are a large family of naturally occurring polyketides exhibiting remarkable anticancer activities. The first generation of annonaceous acetogenin mimetic (1, AA005) exhibits comparable activity as that of natural products and presents much higher selectivity between cancer and normal cells. In this work, we report the design, synthesis, and evaluation of a new series of compound 1 analogues in which a variety of conformation- constrained fragments were embedded in the left hydrocarbon chain part. Compound 7 bearing a biphenyl moiety was identified to exhibit more potent antiproliferative activity and preferentially target cancer cells over normal cells and thus represents a new lead for further optimization.

Original languageEnglish (US)
Pages (from-to)525-533
Number of pages9
JournalJournal of Medicinal Chemistry
Volume54
Issue number2
DOIs
StatePublished - Jan 27 2011

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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