Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones:: Novel p38 MAP kinase inhibitors

被引：40

作者：

Laufer, Stefan A. ^{[1
]}

Ahrens, Gabriele M. ^{[1
]}

Karcher, Solveigh C. ^{[1
]}

Hering, Joerg S. ^{[1
]}

Niess, Raimund ^{[1
]}

机构：

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 26期

关键词：

D O I：

10.1021/jm061072p

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The pathogenesis of chronic inflammatory diseases is promoted by various pro-inflammatory cytokines. p38 MAP kinase seems to be a valid target as it controls proinflammatory cytokine levels on both transcriptional and translational levels. Starting from benzophenone-type inhibitors, a rigidisation strategy lead to 3-amino-6,11-dihydro-dibenzo[b,e]thiepin-11-one, phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones, and dibenzo[a,d]cyclohepten-5-ones. Synthesis, p38 inhibition, and CYP-inhibition of selected compounds are described.

引用

页码：7912 / 7915

页数：4

共 3 条

[1] 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
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (10) : 3074 - 3077
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20TH INTERNATIONAL ELECTRONIC CONFERENCE ON SYNTHETIC ORGANIC CHEMISTRY (ECSOC), 2016,
[3] Metabolically Stable Dibenzo[b,e]oxepin-11(6H)-ones as Highly Selective p38 MAP Kinase Inhibitors: Optimizing Anti-Cytokine Activity in Human Whole Blood
Baur, Benjamin
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JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (21) : 8561 - 8578

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