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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…

文献索引: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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被引用次数: 19

摘要

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.