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

Wan SB; Landis Piwowar KR; Kuhn DJ; Chen D; Dou QP; Chan TH

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

机译：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结构活性研究。

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摘要

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.

机译：已经研究了涉及表皮-没食子儿茶素没食子酸酯（EGCG）的A环和B环的修饰的许多合成绿茶多酚类似物作为蛋白酶体抑制剂的结构-活性关系。发现在B环中，OH基团数目的减少导致效力降低。将疏水苄基引入A环的8位不会显着影响蛋白酶体的抑制能力。

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来源
《Bioorganic and Medicinal Chemistry》 |2005年第6期|P.2177-2185|共9页
作者
Wan SB; Landis Piwowar KR; Kuhn DJ; Chen D; Dou QP; Chan TH;
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作者单位

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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原文格式 PDF
正文语种 eng
中图分类基础医学;
关键词
multicatalytic endopeptidase complex; gallocatechin gallate; inhibitors;

机译：多催化内肽酶复合物;没食子儿茶素没食子酸酯;抑制剂;

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1. Structure-activity relationships of synthetic analogs of (-)-epigallocatechin-3-gallate as proteasome inhibitors. [J] . Kazi A, Wang Z, Kumar N, Anticancer Research: International Journal of Cancer Research and Treatment . 2004,第2B期

机译：（-）-epigallocatechin-3-gallate作为蛋白酶体抑制剂的合成类似物的构效关系。
2. Semi-synthesis and proteasome inhibition of D-ring deoxy analogs of (-)-epigailocatechin gallate (EGCG), the active ingredient of green tea extract [J] . Congde Huo, Guoqing Shi, Wai Har Lam Canadian Journal of Chemistry . 2008,第6期

机译：半合成和蛋白酶体抑制绿茶提取物的有效成分（-）-表儿茶素没食子酸酯（EGCG）的D环脱氧类似物
3. Semi-synthesis and proteasome inhibition of D-ring deoxy analogs of (-)-epigallocatechin gallate (EGCG), the active ingredient of green tea extract [J] . Congde Huo Guoqing Shi Wai Har Lam Di Chen Quizhi Cindy Cui Q. Ping Dou Canadian Journal of Chemistry . 2008,第6期

机译：半合成和蛋白酶体抑制（-）-表没食子儿茶素没食子酸酯（EGCG）的D环脱氧类似物，绿茶提取物的活性成分
4. In vitro study on the metabolism of epigallocatechin gallate (EGCG) in mouse's tissues [C] . Jian Ge, Yang Liu, Meng-xin Wang, International Symposium on Information Technologies in Medicine and Education;ITME 2012 . 2012

机译：表没食子儿茶素没食子酸酯（EGCG）在小鼠组织中代谢的体外研究
5. Synthesis of B-Lactam Belactosin A Analogs as Potential 20S Proteasome Inhibitors. [D] . Harmon, Chelsea R. 2017

机译：B-内酰胺Belactosin A类似物的合成作为潜在的20S蛋白酶体抑制剂。
6. In Vitro Evaluation of the Antiviral Activity of the Synthetic Epigallocatechin Gallate Analog-Epigallocatechin Gallate (EGCG) Palmitate against Porcine Reproductive and Respiratory Syndrome Virus [O] . Chunjian Zhao, Shuaihua Liu, Chunying Li, 2014

机译：合成表没食子儿茶素没食子酸酯类似物-表没食子儿茶素没食子酸酯（EGCG）棕榈酸酯对猪繁殖与呼吸综合征病毒的抗病毒活性的体外评估。
7. Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors [O] . Wan SB, Landis-Piwowar KR, Kuhn DJ, 2005

机译：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结构活性研究

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

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