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

Michael J Munchhof; Jean S Beebe; Jeffery M Casavant; Beth A Cooper; Jonathan L Doty; R Carla Higdon; Stephen M Hillerman; Catherine I Soderstrom; Elisabeth A Knauth; Matthew A Marx; Ann Marie K Rossi; Susan B Sobolov; Jianmin Sun

doi:10.1016/j.bmcl.2003.10.030

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

Bioorg Med Chem Lett. 2004 Jan 5;14(1):21-4. doi: 10.1016/j.bmcl.2003.10.030.

Authors

Michael J Munchhof¹, Jean S Beebe, Jeffery M Casavant, Beth A Cooper, Jonathan L Doty, R Carla Higdon, Stephen M Hillerman, Catherine I Soderstrom, Elisabeth A Knauth, Matthew A Marx, Ann Marie K Rossi, Susan B Sobolov, Jianmin Sun

Affiliation

¹ Pfizer Global Research and Development, Groton Laboratories MS8220-2405, Eastern Point Road, Groton, CT 06340, USA. michael_j_munchhof@groton.pfizer.com

PMID: 14684289
DOI: 10.1016/j.bmcl.2003.10.030

Abstract

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.

MeSH terms

Drug Design
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
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

Substances

Enzyme Inhibitors
Pyridines
Pyrimidines
thienopyridine
thienopyrimidine
Vascular Endothelial Growth Factor Receptor-2