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Novel flavonoids with antiproliferative activities against breast cancer cells.

ABSTRACT: A series of flavone analogues were synthesized and evaluated for their antiproliferation activity against breast cancer cells. The IC(50) of compound 10 and 24 were determined to be at 5 ?M. 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 (IC(50) = 1 ?M) 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.

SUBMITTER: Yao N

PROVIDER: S-EPMC3169196 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature

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Novel flavonoids with antiproliferative activities against breast cancer cells.

Yao Nianhuan N Chen Chao-Yu CY Wu Chun-Yi CY Motonishi Kiyomi K Kung Hsing-Jien HJ Lam Kit S KS

Journal of medicinal chemistry 20110608 13

A series of flavone analogues were synthesized and evaluated for their antiproliferation activity against breast cancer cells. The IC(50) 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 (IC(50) = 1 ...[more]

PMID: 21599001

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