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

Sheng Biao Wan, Kristin R Landis-Piwowar, Deborah J Kuhn, Di Chen, Q Ping Dou, Tak Hang Chan
Bioorganic & Medicinal Chemistry 2005 March 15, 13 (6): 2177-85
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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