Novel cinnoline-based inhibitors of LRRK2 kinase activity.
Bioorg Med Chem Lett
; 23(1): 71-4, 2013 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-23219325
ABSTRACT
Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of cinnoline-3-carboxamides that are potent against both wild-type and mutant LRRK2 kinase activity in biochemical assays. These compounds are also shown to be potent inhibitors in a cellular assay and to have good to excellent CNS penetration.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Proteínas Serina-Treonina Quinasas
/
Inhibidores de Proteínas Quinasas
/
Compuestos Heterocíclicos con 2 Anillos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article
País de afiliación:
Estados Unidos