Novel heterocycle-substituted pyrimidines as inhibitors of NF-κB transcription regulation related to TNF-α cytokine release

被引：15

作者：

Ha, Hyung-Ho ^{[1
]}

Kim, Jee Seon ^{[1
]}

Kim, B. Moon ^{[1
]}

机构：

[1] Seoul Natl Univ, Dept Chem, Seoul 151747, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 02期

关键词：

glycogen synthase kinase 3 beta; nuclear factor kappa B; anti-inflammation; TNF-alpha cytokine; heterocyclic fused ring;

D O I：

10.1016/j.bmcl.2007.11.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel heterocyclic ring-substituted pyrimidines have been designed as inhibitors of glycogen synthase kinase-3 beta (GSK-3P) from the modification of known inhibitors. Several potent inhibitors exhibiting nanomolar activities were discovered against GSK-3 beta kinase as well as in an NF-kappa B reporter gene assay. Based on the results from in vitro TNF-alpha release inhibition and in vivo endotoxima, these inhibitors are expected to be useful candidates for treatment of inflammation-related diseases. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：653 / 656

页数：4

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