Structure-activity relationship studies of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate:: an inhibitor of AP-1 and NF-κB mediated gene expression

被引：40

作者：

Palanki, MSS ^{[1
]}

Gayo-Fung, LM ^{[1
]}

Shevlin, GI ^{[1
]}

Erdman, P ^{[1
]}

Sato, M ^{[1
]}

Goldman, M ^{[1
]}

Ransone, LJ ^{[1
]}

Spooner, C ^{[1
]}

机构：

[1] Celgene Signal Res Div, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(02)00517-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several analogues of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate (1) were synthesized and tested as inhibitors of AP-1 and NF-kappaB mediated transcriptional activation in Jurkat T cells. From our SAR work, ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))-N-methylamino]-4-(trifluoromethyl)-pyrimidine-5-carboxylate was identified as a novel and potent inhibitor. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2573 / 2577

页数：5

共 16 条

[1] Erythromycin suppresses nuclear factor-κB and activator protein-1 activation in human bronchial epithelial cells [J].