1.
Bioorg Med Chem Lett
; 25(18): 3788-92, 2015 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26259804
RESUMO
A series of structure based drug design hypotheses and focused screening efforts led to the identification of tetrahydropyrrolo-diazepenones with striking potency against ERK2 kinase. The role of fluorination in mitigating microsomal clearance was systematically explored. Ultimately, it was found that fluorination of a cyclopentanol substructure provided significant improvement in both potency and human metabolic stability.