Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors

被引：47
|
作者：
Wan, SB
Landis-Piwowar, KR
Kuhn, DJ
Chen, D
Dou, QP
Chan, TH [1 ]
机构：
[1] Hong Kong Polytech Univ, Inst Mol Technol Drug Discovery & Synth, Dept Appl Biol & Chem Technol, Hong Kong, Hong Kong, Peoples R China
[2] Hong Kong Polytech Univ, Inst Mol Technol Drug Discovery & Synth, Open Lab Chirotechnol, Hong Kong, Hong Kong, Peoples R China
[3] Wayne State Univ, Prevent Program, Barbara Ann Karmanos Canc Inst, Sch Med, Detroit, MI USA
[4] Wayne State Univ, Dept Pathol, Sch Med, Detroit, MI USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 06期
基金：
美国国家卫生研究院;
关键词：
D O I：
10.1016/j.bmc.2004.12.056
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：
The structure-activity relationship of a number of synthetic green tea polyphenol analogs involving modifications of A ring and B ring of epi-gallocatechin gallate (EGCG) as proteasome inhibitors has been examined. It was found that in B ring, a decrease in the number of OH groups led to decreased potency. Introduction of a hydrophobic benzyl group into the 8 position of A ring did not significantly affect the proteasome-inhibitory potency. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2177 / 2185
页数：9
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