Discovery of amido-benzisoxazoles as potent c-Kit inhibitors

Autor:	Roland Burli, Matthew H. Plant, Randall W. Hungate, Roxanne Kunz, Douglas A. Whittington, Yang Xu, Shannon Rumfelt, Gordon Ng, Violeta Yu, Michael Schrag, Ning Chen, Yen Nguyen, Yanyan Tudor, Andrew Tasker, Kristin Meagher, Essa Hu, Dawei Zhang
Rok vydání:	2008
Předmět:	medicine.medical_treatment Clinical Biochemistry Molecular Conformation Pharmaceutical Science Crystallography X-Ray p38 Mitogen-Activated Protein Kinases Biochemistry Receptor tyrosine kinase Targeted therapy Structure-Activity Relationship Drug Discovery medicine Combinatorial Chemistry Techniques Humans Structure–activity relationship Tyrosine Molecular Biology Molecular Structure biology Chemistry Kinase Organic Chemistry Receptor Protein-Tyrosine Kinases Isoxazoles Mast cell Amides Proto-Oncogene Proteins c-kit medicine.anatomical_structure Enzyme inhibitor biology.protein Cancer research Molecular Medicine Signal transduction
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:5115-5117
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cdd2f15cb2f6855f01eb5d331d0b8302 https://doi.org/10.1016/j.bmcl.2008.07.111 Zobrazit plný text záznamu Full Text from ScienceDirect