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

Stéphane Raeppel | Zendy; Frédéric Gaudette | Zendy; Hannah Nguyen | Zendy; Normand Beaulieu | Zendy; James Wang | Zendy; Christiane R. Maroun | Zendy; Jeffrey M. Besterman | Zendy; Arkadii Vaisburg | Zendy

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

Author(s) -

Stéphane Raeppel,

Frédéric Gaudette,

Hannah Nguyen,

Normand Beaulieu,

James Wang,

Christiane R. Maroun,

Jeffrey M. Besterman,

Arkadii Vaisburg

Publication year - 2012

Publication title -

international journal of medicinal chemistry

Language(s) - English

Resource type - Journals

eISSN - 2090-2069

pISSN - 2090-2077

DOI - 10.1155/2012/412614

Subject(s) - tropomyosin receptor kinase a , tyrosine kinase , identification (biology) , ror1 , receptor tyrosine kinase , tropomyosin receptor kinase c , receptor , computational biology , pharmacology , biology , platelet derived growth factor receptor , biochemistry , neurotrophin , botany , growth factor

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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