Literature DB >> 19896842

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

Oscar Saavedra1, 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.   

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.

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Year:  2009        PMID: 19896842     DOI: 10.1016/j.bmcl.2009.10.095

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Synthesis of multicyclic pyridine and quinoline derivatives via intramolecular C-H bond functionalization.

Authors:  Sirilata Yotphan; Robert G Bergman; Jonathan A Ellman
Journal:  Org Lett       Date:  2010-07-02       Impact factor: 6.005

2.  1-aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as VEGFR-2 tyrosine kinase inhibitors: synthesis, biological evaluation, and molecular modelling studies.

Authors:  Pedro Soares; Raquel Costa; Hugo J C Froufe; Ricardo C Calhelha; Daniela Peixoto; Isabel C F R Ferreira; Rui M V Abreu; Raquel Soares; Maria-João R P Queiroz
Journal:  Biomed Res Int       Date:  2013-07-07       Impact factor: 3.411

  2 in total

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