Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors

A novel series of N-(3-(6-substituted-aminopyridin-3-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting TrkA receptor tyrosine kinase was identified. SAR study of the series allowed us to design and synthesize compounds possessing inhibitory activity of TrkA kinase enzyme in the low...

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Detalles Bibliográficos
Autores principales: Raeppel, Stéphane L., Gaudette, Frédéric, Nguyen, Hannah, Beaulieu, Normand, Wang, James, Maroun, Christiane, Besterman, Jeffrey M., Vaisburg, Arkadii
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2012
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4412093/
https://www.ncbi.nlm.nih.gov/pubmed/25954527
http://dx.doi.org/10.1155/2012/412614
Descripción
Sumario:A novel series of N-(3-(6-substituted-aminopyridin-3-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting TrkA receptor tyrosine kinase was identified. SAR study of the series allowed us to design and synthesize compounds possessing inhibitory activity of TrkA kinase enzyme in the low nanomolar range with low residual activity against c-Met and with no significant activity against VEGFR2.

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