Serendipity in discovery of proteasome inhibitors

被引：4

作者：

Dunn, Derek ^{[1
]}

Iqbal, Mohamed ^{[1
]}

Husten, Jean ^{[1
]}

Ator, Mark A. ^{[1
]}

Chatterjee, Sankar ^{[1
]}

机构：

[1] Cephalon Inc, W Chester, PA 19380 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 10期

关键词：

Proteasome; Peptidomimetic; Cancer; 20S PROTEASOME; PROTEOLYTIC PATHWAY; CANCER; POTENT; EXPRESSION; BORTEZOMIB; RESOLUTION; APOPTOSIS; SYSTEM;

D O I：

10.1016/j.bmcl.2012.03.086

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Among its various catalytic activities, the 'chymotrypsin-like' activity of the proteasome, a large multicatalytic proteinase complex has emerged as the focus of drug discovery efforts in cancer therapy. Herein, a series of first generation (2S, 3R)-2-amino-3-hydroxybutyric acid derived proteasome inhibitors that were discovered serendipitously en route to original goal of generating a series of sterically constrained oxazoline derivatives has been reported. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3503 / 3505

页数：3

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