- N3-arylmalonamides: a new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases.
N3-arylmalonamides: a new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases.
Bioorganic & medicinal chemistry letters (2009-11-10)
Oscar Saavedra, Stephen Claridge, Lijie Zhan, Franck Raeppel, Marie-Claude Granger, Stéphane Raeppel, Michael Mannion, Frédéric Gaudette, Nancy Zhou, Ljubomir Isakovic, Naomy Bernstein, Robert Déziel, Hannah Nguyen, Normand Beaulieu, Carole Beaulieu, Isabelle Dupont, James Wang, A Robert Macleod, Jeffrey M Besterman, Arkadii Vaisburg
PMID19896842
ABSTRACT
A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC(50) values in the low nanomolar range in vitro and were efficacious in human tumor xenograft models in mice in vivo.
MATERIALS