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

doi:10.1021/jm101440r

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 journal › Article › peer-review

47 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 language	English
Pages (from-to)	4339-4349
Number of pages	11
Journal	Journal of Medicinal Chemistry
Volume	54
Issue number	13
DOIs	https://doi.org/10.1021/jm101440r
Publication status	Published - Jul 14 2011
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm101440r

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title = "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 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.",

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doi = "10.1021/jm101440r",

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T1 - Novel flavonoids with antiproliferative activities against breast cancer cells

AU - Yao, Nianhuan

AU - Chen, Chao Yu

AU - Wu, Chun Yi

AU - Motonishi, Kiyomi

AU - Kung, Hsing Jien

AU - Lam, Kit S.

PY - 2011/7/14

Y1 - 2011/7/14

N2 - 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.

AB - 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.

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JO - Journal of Medicinal Chemistry

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IS - 13

ER -

Novel flavonoids with antiproliferative activities against breast cancer cells

Abstract

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ASJC Scopus subject areas

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