| Literature DB >> 16973359 |
Yonghan Hu1, Neal Green, Lori K Gavrin, Kristin Janz, Neelu Kaila, Huan-Qiu Li, Jennifer R Thomason, John W Cuozzo, J Perry Hall, Sang Hsu, Cheryl Nickerson-Nutter, Jean-Baptiste Telliez, Lih-Ling Lin, Steve Tam.
Abstract
The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tpl2 kinase are described. Potent inhibitors of Tpl2 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificity in cell-based phosphorylation assays in LPS-treated human monocytes were identified. Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNFalpha release when administered intraperitoneally in mice.Entities:
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Year: 2006 PMID： 16973359 DOI： 10.1016/j.bmcl.2006.08.102
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823