N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazoli dine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.

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Raeppel S, Claridge S, Saavedra O, Gaudette F, Zhan L, Mannion M, Zhou N, Raeppel F, Granger MC, Isakovic L, Deziel R, Nguyen H, Beaulieu N, Beaulieu C, Dupont I, Robert MF, Lefebvre S, Dubay M, Rahil J, Wang J, Ste-Croix H, Robert Macleod A, Besterman J, Vaisburg A

N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazoli dine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1323-8. doi: 10.1016/j.bmcl.2009.01.068. Epub 2009 Jan 27.

PubMed ID

19211249 [ View in PubMed

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Abstract

A series of N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazoli dine-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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sunitinib	Vascular endothelial growth factor receptor 2	IC 50 (nM)	185	N/A	N/A	Details