Discovery of amido-benzisoxazoles as potent c-Kit inhibitors

Bioorganic & Medicinal Chemistry Letters
Roxanne K KunzEssa Hu

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.

References

Jul 18, 2002·Nature Reviews. Drug Discovery·Renaud CapdevilleAlex Matter
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Jun 26, 2003·The Journal of Biological Chemistry·Clifford D MolDuncan E McRee
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Dec 31, 2004·Stem Cells·Johan LennartssonR Shivakrupa
Jun 17, 2008·Bioorganic & Medicinal Chemistry Letters·Ning ChenEssa Hu

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Citations

Dec 1, 2011·Journal of Molecular Modeling·Anna Maria AlmericoAntonino Lauria
Nov 8, 2013·Organic Letters·Valentina MercalliGian Cesare Tron

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