| Literature DB >> 16750367 |
Mark Sabat1, John C Vanrens, Michael P Clark, Todd A Brugel, Jennifer Maier, Roger G Bookland, Matthew J Laufersweiler, Steven K Laughlin, Adam Golebiowski, Biswanath De, Lily C Hsieh, Richard L Walter, Marlene J Mekel, Michael J Janusz.
Abstract
A series of C-2, C-8, and N-9 trisubstituted purine based inhibitors of TNF-alpha production are described. The most potent analogs showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell based assay. The SAR of the series was optimized with the aid of X-ray co-crystal structures of these inhibitors bound with mutated p38 (mp38).Entities:
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Year: 2006 PMID： 16750367 DOI： 10.1016/j.bmcl.2006.05.050
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823