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新型四氢-β-咔啉-1-羧酸作为丝裂原活化蛋白激酶激活的蛋白激酶2（MK-2）的抑制剂

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

作者信息

Trujillo John I, Meyers Marvin J, Anderson David R, Hegde Shridhar, Mahoney Matthew W, Vernier William F, Buchler Ingrid P, Wu Kun K, Yang Syaulan, Hartmann Susan J, Reitz David B

机构信息

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

出版信息

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4657-63. doi: 10.1016/j.bmcl.2007.05.070. Epub 2007 May 25.

DOI:10.1016/j.bmcl.2007.05.070
PMID:17570666
Abstract

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.

摘要

对一系列四氢-β-咔啉-1-羧酸类似物进行了构效关系研究，以确定对丝裂原活化蛋白激酶激活的蛋白激酶2（MK-2）具有活性的关键官能团。进一步评估了这些化合物在U937细胞和体内抑制肿瘤坏死因子α（TNFα）产生的能力。这些化合物代表了一类新型的化合物结构类型，能够以显著的选择性抑制MK-2。

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