Novel flavonoids with antiproliferative activities against breast cancer cells

Nianhuan Yao, Chao Yu Chen, Chun Yi Wu, Kiyomi Motonishi, Hsing-Jien Kung, Kit Lam

Research output: Contribution to journalArticle

30 Scopus citations

Abstract

A series of flavone analogues were synthesized and evaluated for their antiproliferation activity against breast cancer cells. The IC50 of compound 10 and 24 were determined to be at 5 μM. These compounds were used as baits to screen breast cancer cDNA expression phage display proteome library. DNA sequencing of the binding phages suggests that eEF1A1 is a target protein for 10 and 24. Further optimization of these compounds led to the discovery of 39 with higher cytotoxic potency (IC50 = 1 μM) and binding to eEF1A2. Biological and biochemical data suggest that eEF1A2 might be a therapeutic target and that 39 is an excellent lead compound for further development.

Original languageEnglish (US)
Pages (from-to)4339-4349
Number of pages11
JournalJournal of Medicinal Chemistry
Volume54
Issue number13
DOIs
StatePublished - Jul 14 2011

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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