Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.

Article Details

Citation

Copy to clipboard

Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Burli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E

Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5115-7. doi: 10.1016/j.bmcl.2008.07.111. Epub 2008 Jul 31.

PubMed ID

18723346 [ View in PubMed

]

Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
6-chloro-N-pyrimidin-5-yl-3-{[3-(trifluoromethyl)phenyl]amino}-1,2-benzisoxazole-7-carboxamide	Vascular endothelial growth factor receptor 2	IC 50 (nM)	353	N/A	N/A	Details