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

A series of N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3- phenylimi dazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC50 values in the low nanomolar range in vitro, posse...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-03, Vol.19 (5), p.1323-1328
Hauptverfasser: Raeppel, Stephane, Claridge, Stephen, Saavedra, Oscar, Gaudette, Frederic, Zhan, Lijie, Mannion, Michael, Zhou, Nancy, Raeppel, Franck, Granger, Marie-Claude, Isakovic, Ljubomir, Deziel, Robert, Nguyen, Hannah, Beaulieu, Normand, Beaulieu, Carole, Dupont, Isabelle, Robert, Marie-France, Lefebvre, Sylvain, Dubay, Marja, Rahil, Jubrail, Wang, James, Ste-Croix, Helene, MacLeod, A Robert, Besterman, Jeffrey, Vaisburg, Arkadii
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:A series of N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3- phenylimi dazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC50 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.01.068