Bioorganic and Medicinal Chemistry Letters p. 4657 - 4663 (2007)
Update date:2022-09-26
Topics:
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.
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.
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