2. Academic Validation
  3. N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors

N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6552-6. doi: 10.1016/j.bmcl.2009.10.040.
Michael Mannion 1,  Stéphane Raeppel,  Stephen Claridge,  Nancy Zhou,  Oscar Saavedra,  Ljubomir Isakovic,  Lijie Zhan,  Frédéric Gaudette,  Franck Raeppel,  Robert Déziel,  Normand Beaulieu,  Hannah Nguyen,  Ian Chute,  Carole Beaulieu,  Isabelle Dupont,  Marie-France Robert,  Sylvain Lefebvre,  Marja Dubay,  Jubrail Rahil,  James Wang,  Hélène Ste-Croix,  A Robert Macleod,  Jeffrey M Besterman,  Arkadii Vaisburg
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, MethylGene Inc, Montréal, QC, Canada.
PMID: 19854051 DOI: 10.1016/j.bmcl.2009.10.040
Abstract

A series of N-(4-(6,7-disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two Enzymes with IC(50) values in the low nanomolar range in vitro, possessed favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice.

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