表没食子儿茶素没食子酸酯（EGCG）类似物作为蛋白酶体抑制剂的构效关系研究。
Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors.
作者信息
Wan Sheng Biao, Landis-Piwowar Kristin R, Kuhn Deborah J, Chen Di, Dou Q Ping, Chan Tak Hang
机构信息
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.
出版信息
Bioorg Med Chem. 2005 Mar 15;13(6):2177-85. doi: 10.1016/j.bmc.2004.12.056.
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.
已经研究了多种合成绿茶多酚类似物的构效关系，这些类似物涉及表没食子儿茶素没食子酸酯（EGCG）的A环和B环修饰作为蛋白酶体抑制剂。研究发现，在B环中，OH基团数量的减少导致活性降低。在A环的8位引入疏水苄基对蛋白酶体抑制活性没有显著影响。
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