Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

被引：285
|
作者：
Anderson, DR
Hegde, S
Reinhard, E
Gomez, L
Vernier, WF
Lee, L
Liu, S
Sambandam, A
Snider, PA
Masih, L
机构：
[1] Pfizer Global Res & Dev, Chesterfield, MO 63017 USA
[2] Albany Mol Res Inc, Albany, NY 12212 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 06期
关键词：
MK-2; kinase inhibitor; TNF alpha;
D O I：
10.1016/j.bmcl.2005.01.067
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported. © 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1587 / 1590
页数：4
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