N 3-Arylmalonamides: A new series of thieno [3, 2-b] pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases

O Saavedra, S Claridge, L Zhan, F Raeppel…

Index: Saavedra, Oscar; Claridge, Stephen; Zhan, Lijie; Raeppel, Franck; Granger, Marie-Claude; Raeppel, Stephane; Mannion, Michael; Gaudette, Frederic; Zhou, Nancy; Isakovic, Ljubomir; Bernstein, Naomy; Deziel, Robert; Nguyen, Hannah; Beaulieu, Normand; Beaulieu, Carole; Dupont, Isabelle; Wang, James; Macleod, A. Robert; Besterman, Jeffrey M.; Vaisburg, Arkadii Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 24 p. 6836 - 6839

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Citation Number: 19

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 IC50 values in the low nanomolar range in vitro and were efficacious in human tumor xenograft models in mice in vivo.