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

页码：2177 / 2185

页数：9

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