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

…, MW Mahoney, RG Kurumbail, N Caspers…

Index: Anderson, David R.; Meyers, Marvin J.; Vernier, William F.; Mahoney, Matthew W.; Kurumbail, Ravi G.; Caspers, Nicole; Poda, Gennadiy I.; Schindler, John F.; Reitz, David B.; Mourey, Robert J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2647 - 2654

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Citation Number: 137

Abstract

A new class of potent kinase inhibitors selective for mitogen-activated protein kinase- activated protein kinase 2 (MAPKAP-K2 or MK-2) for the treatment of rheumatoid arthritis has been prepared and evaluated. These inhibitors have IC50 values as low as 10 nM against the target and have good selectivity profiles against a number of kinases including CDK2, ERK, JNK, and p38. These MK-2 inhibitors have been shown to suppress TNFα ...