Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
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.
Humphries
Paul S
PS
Pfizer Global R&D, San Diego, CA 92121, USA. phumphri@gmail.com
Lafontaine
Jennifer A
JA
Agree
Charles S
CS
Alexander
David
D
Chen
Ping
P
Do
Quyen-Quyen T
QQ
Li
Lilian Y
LY
Lunney
Elizabeth A
EA
Rajapakse
Ranjan J
RJ
Siegel
Karen
K
Timofeevski
Sergei L
SL
Wang
Tianlun
T
Wilhite
David M
DM