Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).
J Med Chem
; 53(3): 1383-6, 2010 Feb 11.
Article
em En
| MEDLINE
| ID: mdl-20030343
ABSTRACT
Class III histone deacetylases (sirtuins) play pivotal roles in many cellular processes. They are linked to extended lifespan and to the pathogenesis of cancer and neuronal disorders. We present novel sirtuin inhibitors based on a 6,7-dichloro-2-oxindole scaffold with low micromolar activity. In vitro activity was rationalized by docking studies, and hyperacetylation of sirtuin targets could be demonstrated in cell culture.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sirtuínas
/
Inibidores de Histona Desacetilases
/
Indóis
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article