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Bioorg Med Chem Lett ; 18(9): 2793-8, 2008 May 01.
Article in English | MEDLINE | ID: mdl-18434145

ABSTRACT

A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 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.


Subject(s)
Antineoplastic Agents/pharmacology , Cell Division/drug effects , Protein Kinase Inhibitors/pharmacology , Proto-Oncogene Proteins c-met/antagonists & inhibitors , Pyridines/pharmacology , Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors , Animals , Antineoplastic Agents/chemical synthesis , Humans , Mice , Models, Chemical , Protein Kinase Inhibitors/chemical synthesis , Pyridines/chemical synthesis , Structure-Activity Relationship , Tumor Cells, Cultured , Xenograft Model Antitumor Assays
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