Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Bioorg Med Chem Lett
; 20(24): 7303-7, 2010 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-21071223
ABSTRACT
From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards closely related MAP kinases p38 and Erk2. Herein we describe the evolution of these compounds to a novel class of thiophene and thiazole JNK inhibitors that retain favorable solubility, permeability, and P-gp properties for development as CNS agents for treatment of neurodegeneration. Compound 61 demonstrated JNK3 IC(50)=77 nM and retained the excellent broad kinase selectivity observed for the series.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinolinas
/
Tiazóis
/
Tiofenos
/
Proteínas Quinases JNK Ativadas por Mitógeno
/
Inibidores de Proteínas Quinases
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article