3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: Synthesis and initial structure-activity relationships

被引：39

作者：

Dhar, TGM ^{[1
]}

Shen, ZQ ^{[1
]}

Gu, HH ^{[1
]}

Chen, P ^{[1
]}

Norris, D ^{[1
]}

Watterson, SH ^{[1
]}

Ballentine, SK ^{[1
]}

Fleener, CA ^{[1
]}

Rouleau, KA ^{[1
]}

Barrish, JC ^{[1
]}

Townsend, R ^{[1
]}

Hollenbaugh, DL ^{[1
]}

Iwanowicz, EJ ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(03)00757-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH), based upon a 3-cyanoindole core, were explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SAR), derived from in vitro studies, for this new series of inhibitors is given. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3557 / 3560

页数：4

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