Design, synthesis and SAR of phenylamino-substituted 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones and 11H-dibenzo[b,f]oxepin-10-ones as p38 MAP kinase inhibitors

被引：25

作者：

Dorn, Angelika ^{[1
]}

Schattel, Verena ^{[1
]}

Laufer, Stefan ^{[1
]}

机构：

[1] Univ Tubingen, Inst Pharm, Dept Pharmaceut & Med Chem, D-72076 Tubingen, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 10期

关键词：

Kinase inhibitors; Linear binders; DERIVATIVES; PROTEIN; ARTHRITIS; BINDING; ACIDS;

D O I：

10.1016/j.bmcl.2010.03.107

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The p38 MAP kinase is a key enzyme in inflammatory diseases as it is involved in the biosynthesis of proinflammatory cytokines such as TNF-alpha and IL-1 beta. Small molecule p38 inhibitors suppress the production of these cytokines and therefore p38 is a promising drug target for novel anti-inflammatory therapeutics. In this study, we report the design, synthesis, and SAR of novel N-substituted 11H-dibenzo[b,f]oxepin-10-ones and 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones as p38 inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3074 / 3077

页数：4

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