Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.
A series of dianilinopyrimidineureas demonstrate potency as VEGFR2 kinase inhibitors.
GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA. douglas.m.sammond@gsk.com
Douglas M
DM
Sammond
Kristen E
KE
Nailor
James M
JM
Veal
Robert T
RT
Nolte
Liping
L
Wang
Victoria B
VB
Knick
Sharon K
SK
Rudolph
Anne T
AT
Truesdale
Eldridge N
EN
Nartey
Jeffrey A
JA
Stafford
Rakesh
R
Kumar
Mui
M
Cheung
D000814:Aniline Compounds / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000814:Aniline Compounds; D004791:Enzyme Inhibitors; D017320:HIV Protease Inhibitors; D011743:Pyrimidines; C504379:dianilinopyrimidineurea; D014508:Urea; D011505:Protein-Tyrosine Kinases; D040301:Vascular Endothelial Growth Factor Receptor-2; C023650:aniline