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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Published inInternational Journal of Medicinal Chemistry (Online) Vol. 2012; no. 2012; pp. 1 - 6
Main Authors Raeppel, Stéphane L., Gaudette, Frédéric, Nguyen, Hannah, Beaulieu, Normand, Wang, James, Maroun, Christiane, Besterman, Jeffrey M., Vaisburg, Arkadii
Format Journal Article
LanguageEnglish
Published Cairo, Egypt Hindawi Puplishing Corporation 01.01.2012
Hindawi Publishing Corporation
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Summary: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.
Bibliography:Academic Editor: O. Bruno
ISSN:2090-2069
2090-2077
DOI:10.1155/2012/412614