| Literature DB >> 15341957 |
Jennifer A Townes1, Adam Golebiowski, Michael P Clark, Matthew J Laufersweiler, Todd A Brugel, Mark Sabat, Roger G Bookland, Steve K Laughlin, John C VanRens, Biswanath De, Lily C Hsieh, Susan C Xu, Michael J Janusz, Richard L Walter.
Abstract
4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-alpha production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell-based assay and against human p38 alpha MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented.Entities:
Mesh：
Substances：
Year: 2004 PMID： 15341957 DOI： 10.1016/j.bmcl.2004.07.024
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823