Novel tetrahydro-β-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)
A structure-activity relationship study was conducted on a series of tetrahydro-β-carboline-1-carboxylic acid analogs in order to identify the key functionality responsible for activity against the mitogen-activated protein kinase-activated protein kinase 2 enzyme (MK-2). The compounds were further evaluated for their ability to inhibit TNFα production in U937 cells and in vivo. These compounds represent a novel structural class of compounds capable of inhibiting MK-2 with remarkable selectivity.
Trujillo, John I.,Meyers, Marvin J.,Anderson, David R.,Hegde, Shridhar,Mahoney, Matthew W.,Vernier, William F.,Buchler, Ingrid P.,Wu, Kun K.,Yang, Syaluan,Hartmann, Susan J.,Reitz, David B.
p. 4657 - 4663
(2008/02/13)
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