Discovery of amido-benzisoxazoles as potent c-Kit inhibitors
Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors has been shown clinically to successfully treat gastrointestinal stromal tumors and mastocytosis. Targeted therapy of c-Kit activity may provide therapeutic advantages against off-target effects for non-oncology applications. A new structural class of c-Kit inhibitors is described, including in vitro c-Kit potency, kinase selectivity, and the observed binding mode.
Kunz, Roxanne K.,Rumfelt, Shannon,Chen, Ning,Zhang, Dawei,Tasker, Andrew S.,Buerli, Roland,Hungate, Randall,Yu, Violeta,Nguyen, Yen,Whittington, Douglas A.,Meagher, Kristin L.,Plant, Matthew,Tudor, Yanyan,Schrag, Michael,Xu, Yang,Ng, Gordon Y.,Hu, Essa
scheme or table
p. 5115 - 5117
(2009/05/26)
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