Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors |
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| Authors: | Wan Sheng Biao Landis-Piwowar Kristin R Kuhn Deborah J Chen Di Dou Q Ping Chan Tak Hang |
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| Institution: | Department of Applied Biology and Chemical Technology and the Open Laboratory of Chirotechnology, Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, SAR, China. |
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| 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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