title: Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity.
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.
authors.affiliation: Pfizer Global Research and Development, Groton Laboratories MS8220-2405, Eastern Point Road, Groton, CT 06340, USA. michael_j_munchhof@groton.pfizer.com
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Munchhof
authors.forename: Jean S
authors.initials: JS
authors.lastname: Beebe
authors.forename: Jeffery M
authors.initials: JM
authors.lastname: Casavant
authors.forename: Beth A
authors.initials: BA
authors.lastname: Cooper
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Doty
authors.forename: R Carla
authors.initials: RC
authors.lastname: Higdon
authors.forename: Stephen M
authors.initials: SM
authors.lastname: Hillerman
authors.forename: Catherine I
authors.initials: CI
authors.lastname: Soderstrom
authors.forename: Elisabeth A
authors.initials: EA
authors.lastname: Knauth
authors.forename: Matthew A
authors.initials: MA
authors.lastname: Marx
authors.forename: Ann Marie K
authors.initials: AM
authors.lastname: Rossi
authors.forename: Susan B
authors.initials: SB
authors.lastname: Sobolov
authors.forename: Jianmin
authors.initials: J
authors.lastname: Sun
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; D011743:Pyrimidines; C446540:thienopyridine; C476003:thienopyrimidine; D040301:Vascular Endothelial Growth Factor Receptor-2