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

SB Wan, KR Landis-Piwowar, DJ Kuhn, D Chen…

Index: Wan, Sheng Biao; Landis-Piwowar, Kristin R.; Kuhn, Deborah J.; Chen, Di; Dou, Q. Ping; Chan, Tak Hang Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 6 p. 2177 - 2185

Full Text: HTML

Citation Number: 46

Abstract

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.