Synthesis and biological activities of fluorinated chalcone derivatives

被引：71

作者：

Nakamura, C

Kawasaki, N

Miyataka, H

Jayachandran, E

Kim, IH

Kirk, KL

Taguchi, T

Takeuchi, Y

Hori, H

Satoh, T

机构：

[1] Tokushima Bunri Univ, Fac Pharmaceut Sci, Tokushima 7708514, Japan

[2] NIDDKD, Bioorgan Chem Lab, NIH, Bethesda, MD 20892 USA

[3] Tokyo Univ Pharm & Life Sci, Sch Pharm, Tokyo 1920392, Japan

[4] Toyama Med & Pharmaceut Univ, Fac Pharmaceut Sci, Toyama 9300194, Japan

[5] Univ Tokushima, Fac Engn, Dept Biol Sci & Technol, Tokushima 7708506, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 03期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/S0968-0896(01)00319-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We have designed and synthesized new 5-lipoxygenase inhibitors, fluorinated 3,4-dihydroxychalcones, and evaluated their biological activities with respect to antiperoxidation activity and in vitro antitumor activities. All fluorinated chalcones tested showed 5-lipoxygenase inhibition on rat basophilic leukemia-1 (RBL-1) cells and inhibitory action on Fe3+ -ADP induced NADPH-dependent lipid peroxidation in rat liver microsomes. The potencies were comparable or better to that of the lead 3,4-dihydroxychalcone. 6-Fluoro-3,4-dihydroxy-2',4'-dimethoxy chalcone (7) was the most effective compound in the in vitro assay using a human cancer cell line panel (HCC panel) consisting of 39 systems. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：699 / 706

页数：8

共 21 条

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BAI R, 1991, J BIOL CHEM, V266, P15882

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