title: 4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II.
abstract: A series of 4-aminopyrimidine-5-carbaldehyde oxime was discovered to have potent VEGFR-2 inhibitory activity. Described here are the chemistry for analogue synthesis and SAR study results. The PK properties, kinase profiling, and in vivo efficacy study for compound 4b are also discussed.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development LLC, Raritan, NJ 08869, USA. shenlinhuang@hotmail.com
authors.forename: Shenlin
authors.initials: S
authors.lastname: Huang
authors.forename: Ronghua
authors.initials: R
authors.lastname: Li
authors.forename: Kenneth R
authors.initials: KR
authors.lastname: LaMontagne
authors.forename: Lee M
authors.initials: LM
authors.lastname: Greenberger
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
mesh_terms: D000818:Animals; D051379:Mice; D010091:Oximes / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: D010091:Oximes; D040301:Vascular Endothelial Growth Factor Receptor-2