Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38α MAPK inhibitors in Werner syndrome cells

…, PGS Murziani, MJ Rokicki, CS Widdowson…

Index: Davis, Terence; Bagley, Mark C.; Dix, Matthew C.; Murziani, Paola G.S.; Rokicki, Michal J.; Widdowson, Caroline S.; Zayed, Jameel M.; Bachler, Marcus A.; Kipling, David Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 24 p. 6832 - 6835

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Citation Number: 25

Abstract

A benzopyranopyridine inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2) is prepared rapidly and efficiently in one step using microwave dielectric heating, whereas a substrate-selective p38 MAPK inhibitor was prepared using conventional heating techniques. The former had MK2 inhibitory activity above 2.5 μM concentration, whereas the latter showed no MK2 inhibition at 10μM. However, rather than rescuing the reduced ...