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
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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.
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