Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
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 TNFalpha in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.
Anderson
David R
DR
Pfizer Global Research and Development, 700 Chesterfield Parkway W, Chesterfield, MO 63017, USA. david.r.anderson@pfizer.com
Hegde
Shridhar
S
Reinhard
Emily
E
Gomez
Leslie
L
Vernier
William F
WF
Lee
Len
L
Liu
Shuang
S
Sambandam
Aruna
A
Snider
Patricia A
PA
Masih
Liaqat
L
D000818:Animals; D015870:Gene Expression; D006801:Humans; D048370:MAP Kinase Kinase 2 / Q000037:antagonists & inhibitors*; D008956:Models, Chemical; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism; D020298:U937 Cells
D011725:Pyridines; D014409:Tumor Necrosis Factor-alpha; D048370:MAP Kinase Kinase 2