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Novel heterocycle-substituted pyrimidines as inhibitors of NF-kappaB transcription regulation related to TNF-alpha cytokine release.

作者信息

Ha Hyung-Ho, Kim Jee Seon, Kim B Moon

机构信息

Department of Chemistry, Seoul National University, Seoul 151-747, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2008 Jan 15;18(2):653-6. doi: 10.1016/j.bmcl.2007.11.064. Epub 2007 Nov 22.

DOI:10.1016/j.bmcl.2007.11.064
PMID:18054489
Abstract

Novel heterocyclic ring-substituted pyrimidines have been designed as inhibitors of glycogen synthase kinase-3beta (GSK-3beta) from the modification of known inhibitors. Several potent inhibitors exhibiting nanomolar activities were discovered against GSK-3beta kinase as well as in an NF-kappaB 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.

摘要

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