Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 11, Pages 3065-3068Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800188g
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Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR, p38, Lck, and Src. In vivo efficacy of pyridone 16 by dose-dependent inhibition of histamine release was demonstrated in a rodent pharmacodynamic model of mast cell activation.
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