Inhibition of Tpl2 kinase and TNFα production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis
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 TNFα release when administered intraperitoneally in mice.
Hu, Yonghan,Green, Neal,Gavrin, Lori K.,Janz, Kristin,Kaila, Neelu,Li, Huan-Qiu,Thomason, Jennifer R.,Cuozzo, John W.,Hall, J. Perry,Hsu, Sang,Nickerson-Nutter, Cheryl,Telliez, Jean-Baptiste,Lin, Lih-Ling,Tam, Steve
p. 6067 - 6072
(2007/10/03)
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