Document Report Card
Basic Information
ID: ALA1157925
Journal: Bioorg Med Chem Lett
Title: Identification of a novel series of potent RON receptor tyrosine kinase inhibitors.
Authors: Raeppel S, Gaudette F, Mannion M, Claridge S, Saavedra O, Isakovic L, Déziel R, Beaulieu N, Beaulieu C, Dupont I, Nguyen H, Wang J, Macleod AR, Maroun C, Besterman JM, Vaisburg A.
Abstract: A novel series of N-(3-fluoro-4-(2-substituted-thieno[3,2-b]pyridin-7-yloxy)phenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamides targeting RON receptor tyrosine kinase was designed and synthesized. SAR study of the series allowed us to identify compounds possessing either inhibitory activity of RON kinase enzyme in the low nanomolar range with low residual activity against the closely related c-Met or potent dual inhibitory activity against RON and c-Met, with no significant activity against VEGFR2 in both cases.
CiteXplore: 20363625