Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase

被引：22

作者：

Kempson, James ^{[1
]}

Guo, Junqing ^{[1
]}

Das, Jagabandhu ^{[1
]}

Moquin, Robert V. ^{[1
]}

Spergel, Steven H. ^{[1
]}

Watterson, Scott H. ^{[1
]}

Langevine, Charles M. ^{[1
]}

Dyckman, Alaric J. ^{[1
]}

Pattoli, Mark ^{[1
]}

Burke, James R. ^{[1
]}

Yang, XiaoXia ^{[1
]}

Gillooly, Kathleen M. ^{[1
]}

McIntyre, Kim W. ^{[1
]}

Chen, Laishun ^{[1
]}

Dodd, John H. ^{[1
]}

McKinnon, Murray ^{[1
]}

Barrish, Joel C. ^{[1
]}

Pitts, William J. ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Res & Dev, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期

关键词：

IKK; TNF; SAR; LPS; INFLAMMATORY RESPONSES; GENE-EXPRESSION; CELLS; ALPHA; MICE; PROLIFERATION; TRANSCRIPTION; ARTHRITIS; COLLAGEN; POTENT;

D O I：

10.1016/j.bmcl.2009.03.159

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS. Published by Elsevier Ltd.

引用

页码：2646 / 2649

页数：4

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