Novel tetrahydro-β-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

…, S Hegde, MW Mahoney, WF Vernier, IP Buchler…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 16 p. 4657 - 4663

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Citation Number: 102

Abstract

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 ...