2. Academic Validation
  3. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases

Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8. doi: 10.1016/j.bmcl.2008.04.009.
Stephen Claridge 1,  Franck Raeppel,  Marie-Claude Granger,  Naomy Bernstein,  Oscar Saavedra,  Lijie Zhan,  David Llewellyn,  Amal Wahhab,  Robert Deziel,  Jubrail Rahil,  Normand Beaulieu,  Hannah Nguyen,  Isabelle Dupont,  Annie Barsalou,  Carole Beaulieu,  Ian Chute,  Serge Gravel,  Marie-France Robert,  Sylvain Lefebvre,  Marja Dubay,  Roussen Pascal,  Jeff Gillespie,  Zhiyun Jin,  James Wang,  Jeffrey M Besterman,  A Robert MacLeod,  Arkadii Vaisburg
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1. [email protected]
PMID: 18434145 DOI: 10.1016/j.bmcl.2008.04.009
Abstract

A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2/KDR/Flk-1 tyrosine kinases is described. The compounds demonstrated potency with IC(50) values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against various human tumor xenograft models in mice. Further exploration of this class of compounds is underway.

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