1.
Bioorg Med Chem Lett
; 23(5): 1486-92, 2013 Mar 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23352510
RESUMO
A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and selective JNK inhibitor, compound 24f (JNK1 and 2 IC(50)=16 and 66 nM, respectively), with bioavailability in rats and suitable for further in vivo pharmacological evaluation.