Novel flavonoids with antiproliferative activities against breast cancer cells

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

Research output: Contribution to journalArticle

28 Citations (Scopus)

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
Pages (from-to)4339-4349
Number of pages11
JournalJournal of Medicinal Chemistry
Volume54
Issue number13
DOIs
Publication statusPublished - Jul 14 2011
Externally publishedYes

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flavone
Flavonoids
Bacteriophages
Inhibitory Concentration 50
Breast Neoplasms
Proteome
DNA Sequence Analysis
Complementary DNA
Proteins
Therapeutics
Lead
N-dodecyl-L-lysine amide

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Novel flavonoids with antiproliferative activities against breast cancer cells. / Yao, Nianhuan; Chen, Chao Yu; Wu, Chun Yi; Motonishi, Kiyomi; Kung, Hsing Jien; Lam, Kit S.

In: Journal of Medicinal Chemistry, Vol. 54, No. 13, 14.07.2011, p. 4339-4349.

Research output: Contribution to journalArticle

Yao, Nianhuan ; Chen, Chao Yu ; Wu, Chun Yi ; Motonishi, Kiyomi ; Kung, Hsing Jien ; Lam, Kit S. / Novel flavonoids with antiproliferative activities against breast cancer cells. In: Journal of Medicinal Chemistry. 2011 ; Vol. 54, No. 13. pp. 4339-4349.
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