1.
Bioorg Med Chem Lett
; 22(14): 4528-31, 2012 Jul 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-22727637
RESUMEN
Four hinge-binding scaffolds have been explored for novel selective Aurora kinase inhibitors. The structure activity relationship, selectivity and pharmacokinetic profiles have been evaluated.
Asunto(s)
Inhibidores de Proteínas Quinasas/síntesis química , Proteínas Serina-Treonina Quinasas/antagonistas & inhibidores , Animales , Aurora Quinasas , Línea Celular , Ratones , Modelos Moleculares , Estructura Molecular , Inhibidores de Proteínas Quinasas/farmacología , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 21(18): 5620-4, 2011 Sep 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21778056
RESUMEN
In an effort to discover Aurora kinase inhibitors, an HTS hit revealed an amide containing pyrrolopyrimidine compound. Replacement of the pyrrolopyrimidine residue with a thienopyrimidine moiety led to a series of potent and selective Aurora inhibitors.