title: Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
abstract: The development of a series of novel 4-substituted-2-aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, and the in vitro inhibitory value for a c-Jun cellular assay are discussed. Optimization of microsomal clearance led to the identification of 9c, whose kinase selectivity is reported.
authors.affiliation: Pfizer Global R&D, San Diego, CA 92121, USA. phumphri@gmail.com
authors.forename: Paul S
authors.initials: PS
authors.lastname: Humphries
authors.forename: Jennifer A
authors.initials: JA
authors.lastname: Lafontaine
authors.forename: Charles S
authors.initials: CS
authors.lastname: Agree
authors.forename: David
authors.initials: D
authors.lastname: Alexander
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Quyen-Quyen T
authors.initials: QQ
authors.lastname: Do
authors.forename: Lilian Y
authors.initials: LY
authors.lastname: Li
authors.forename: Elizabeth A
authors.initials: EA
authors.lastname: Lunney
authors.forename: Ranjan J
authors.initials: RJ
authors.lastname: Rajapakse
authors.forename: Karen
authors.initials: K
authors.lastname: Siegel
authors.forename: Sergei L
authors.initials: SL
authors.lastname: Timofeevski
authors.forename: Tianlun
authors.initials: T
authors.lastname: Wang
authors.forename: David M
authors.initials: DM
authors.lastname: Wilhite