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International Journal of Medicinal Chemistry
Volume 2012, Article ID 412614, 6 pages
http://dx.doi.org/10.1155/2012/412614
Research Article

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

1Department of Medicinal Chemistry, MethylGene Inc., 7150 Rue Frederick-Banting, Suite 200, Montréal, QC, Canada H4S 2A1
2Department of Cell Biology and Pharmacology, MethylGene Inc., 7150 Rue Frederick-Banting, Suite 200, Montréal, QC, Canada H4S 2A1
3Department of PK/Analytical Chemistry, MethylGene Inc., 7150 Rue Frederick-Banting, Suite 200, Montréal, QC, Canada H4S 2A1

Received 5 December 2011; Revised 13 February 2012; Accepted 13 February 2012

Academic Editor: O. Bruno

Copyright © 2012 Stéphane L. Raeppel et al. 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.

Abstract

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.