The structural requirements for inhibition of proteasome function by the lactacystin-derived β-lactone and synthetic analogs

被引：49

作者：

Corey, EJ ^{[1
]}

Li, WDZ ^{[1
]}

Nagamitsu, T ^{[1
]}

Fenteany, G ^{[1
]}

机构：

[1] Harvard Univ, Dept Chem & Biol Chem, Cambridge, MA 02138 USA

来源：

TETRAHEDRON | 1999年 / 55卷 / 11期

基金：

美国国家科学基金会; 美国国家卫生研究院;

关键词：

D O I：

10.1016/S0040-4020(98)01142-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of analogs of the lactacystin-derived beta-lactone (2) in which the substituents at C(5), C(7) and C(9) were systematically varied has led to a well defined structure-activity correlation for the highly selective inhibition of the mammalian 20 S proteasome. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：3305 / 3316

页数：12

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