Ontology highlight
ABSTRACT:
SUBMITTER: Zheng K
PROVIDER: S-EPMC4394340 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20150302 4
A novel series of 2-aminopyridopyrimidinone based JNK (c-jun N-terminal kinase) inhibitors were discovered and developed. Structure-activity relationships (SARs) were systematically developed utilizing biochemical and cell based assays and in vitro and in vivo drug metabolism and pharmacokinetic (DMPK) studies. Through the optimization of lead compound 1, several potent and selective JNK inhibitors with high oral bioavailability were developed. Inhibitor 13 was a potent JNK3 inhibitor (IC50 = 15 ...[more]