1.
Bioorg Med Chem Lett
; 20(6): 1985-9, 2010 Mar 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20167481
RESUMEN
From an HTS hit, a series of potent and selective inhibitors of GSK3beta have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2.
Asunto(s)
Proteína Quinasa CDC2/antagonistas & inhibidores , Quinasa 2 Dependiente de la Ciclina/antagonistas & inhibidores , Glucógeno Sintasa Quinasa 3/antagonistas & inhibidores , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Diseño de Fármacos , Glucógeno Sintasa Quinasa 3 beta , Modelos Moleculares , Especificidad por Sustrato
2.
Bioorg Med Chem Lett
; 20(7): 2344-9, 2010 Apr 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20189807
RESUMEN
From potent and selective inhibitors of GSK3beta displaying CYP1A2 inhibition and poor PK properties, mostly linked to metabolic instability and in vivo hydrolysis of the amide bond, we were able to obtain safe and orally available inhibitors with good half lives.