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
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author Raeppel, Stéphane L.
Gaudette, Frédéric
Nguyen, Hannah
Beaulieu, Normand
Wang, James
Maroun, Christiane
Besterman, Jeffrey M.
Vaisburg, Arkadii
author_facet Raeppel, Stéphane L.
Gaudette, Frédéric
Nguyen, Hannah
Beaulieu, Normand
Wang, James
Maroun, Christiane
Besterman, Jeffrey M.
Vaisburg, Arkadii
author_sort Raeppel, Stéphane L.
collection PubMed
description 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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spelling pubmed-44120932015-05-07 Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors Raeppel, Stéphane L. Gaudette, Frédéric Nguyen, Hannah Beaulieu, Normand Wang, James Maroun, Christiane Besterman, Jeffrey M. Vaisburg, Arkadii Int J Med Chem Research Article 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. Hindawi Publishing Corporation 2012 2012-05-02 /pmc/articles/PMC4412093/ /pubmed/25954527 http://dx.doi.org/10.1155/2012/412614 Text en Copyright © 2012 Stéphane L. Raeppel et al. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Raeppel, Stéphane L.
Gaudette, Frédéric
Nguyen, Hannah
Beaulieu, Normand
Wang, James
Maroun, Christiane
Besterman, Jeffrey M.
Vaisburg, Arkadii
Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors
title Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors
title_full Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors
title_fullStr Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors
title_full_unstemmed Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors
title_short Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors
title_sort identification of a novel series of potent trka receptor tyrosine kinase inhibitors
topic Research Article
url 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
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