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

被引：24

作者：

Palanki, MSS ^{[1
]}

Erdman, PE ^{[1
]}

Manning, AM ^{[1
]}

Ow, A ^{[1
]}

Ranson, LJ ^{[1
]}

Spooner, D ^{[1
]}

Suto, C ^{[1
]}

Suto, M ^{[1
]}

机构：

[1] Signal Pharmaceut Inc, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(00)00312-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an effort to identify novel inhibitors of AP-1 and NF-kappa B mediated transcriptional activation, several analogues of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)pyrimidine-5-carboxylate (1) were synthesized and tested in two in vitro assays. The 2-(2'-thienyl) substituted compound (II) was identified as the most potent in this series. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：1645 / 1648

页数：4

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