Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity

Novel classes of thienopyrimidines and thienopyridines have been identified as potent inhibitors of VEGFR-2 kinase. The synthesis and SAR of these compounds is presented, along with successful efforts to diminish EGFR activity present in the lead series. Novel thienopyrimidines and thienopyridines h...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-01, Vol.14 (1), p.21-24
Main Authors: Munchhof, Michael J., Beebe, Jean S., Casavant, Jeffery M., Cooper, Beth A., Doty, Jonathan L., Higdon, R.Carla, Hillerman, Stephen M., Soderstrom, Catherine I., Knauth, Elisabeth A., Marx, Matthew A., Rossi, Ann Marie K., Sobolov, Susan B., Sun, Jianmin
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
Medical sciences
Pharmacology. Drug treatments
Pyridines - chemical synthesis
Pyridines - chemistry
Pyridines - pharmacology
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - pharmacology
Structure-Activity Relationship
Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors
Vascular Endothelial Growth Factor Receptor-2 - metabolism
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Summary:Novel classes of thienopyrimidines and thienopyridines have been identified as potent inhibitors of VEGFR-2 kinase. The synthesis and SAR of these compounds is presented, along with successful efforts to diminish EGFR activity present in the lead series. Novel thienopyrimidines and thienopyridines have been identified as potent inhibitors of VEGFR-2 kinase activity. The synthesis and SAR of these compounds is presented, highlighting our successful effort to diminish the EGFR kinase activity in the lead series.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.10.030