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Bioorg Med Chem Lett. 2007 Aug 15;17(16):4657-63. Epub 2007 May 25.

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

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Department of Medicinal Chemistry, Pfizer Global Research and Development, Chesterfield, MO 63017, USA.

Erratum in

  • Bioorg Med Chem Lett. 2009 Apr 15;19(8):2365. Yang, Syaluan [corrected to Yang, Syaulan].


A structure-activity relationship study was conducted on a series of tetrahydro-beta-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 TNFalpha 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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