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. 2006 Dec 1;16(23):6067-72.
doi: 10.1016/j.bmcl.2006.08.102. Epub 2006 Sep 14.

Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis

Yonghan Hu  1 , 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
Affiliations

Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis

Yonghan Hu et al. Bioorg Med Chem Lett. .

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.

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