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