N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases

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

Journal Article

N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases

Bioorganic and Medicinal Chemistry Letters (2009) 19(24) 6836-6839

DOI: 10.1016/j.bmcl.2009.10.095

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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. © 2009 Elsevier Ltd. All rights reserved.

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Saavedra, O., Claridge, S., Zhan, L., Raeppel, F., Granger, M. C., Raeppel, S., … Vaisburg, A. (2009). N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorganic and Medicinal Chemistry Letters, 19(24), 6836–6839. https://doi.org/10.1016/j.bmcl.2009.10.095

N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases

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