Design and synthesis of novel protease inhibitors. Tripeptide alpha',beta'-epoxyketones as nanomolar inactivators of the proteasome.

被引：45

作者：

Spaltenstein, A

Leban, JJ

Huang, JJ

Reinhardt, KR

Viveros, OH

Sigafoos, J

Crouch, R

机构：

[1] BURROUGHS WELLCOME CO,DEPT PHARMACOL,RES TRIANGLE PK,NC 27709

[2] BURROUGHS WELLCOME CO,DIV BIOANALYT SCI,RES TRIANGLE PK,NC 27709

来源：

TETRAHEDRON LETTERS | 1996年 / 37卷 / 09期

关键词：

D O I：

10.1016/0040-4039(96)00018-4

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Tripeptide alpha',beta'-epoxyketones were prepared stereospecifically starting from Boc-[S]-phenylalanine. Diastereomer 5b inhibited the chymotrypsin-like activity of porcine endothelial cell derived proteasome at low nanomolar concentrations.

引用

页码：1343 / 1346

页数：4

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