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N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases |
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| Authors: | 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 |
| Institution: | 1. Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, QC, Canada H4S 2A1;2. Department of Biology, 7220 Frederick-Banting, Montréal, QC, Canada H4S 2A1;3. Department of PK/Analytical Chemistry, 7220 Frederick-Banting, Montréal, QC, Canada H4S 2A1 |
| Abstract: | A family of thieno3,2-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. |
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