The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.
Bioorg Med Chem Lett
; 17(19): 5300-9, 2007 Oct 01.
Article
en En
| MEDLINE
| ID: mdl-17761416
ABSTRACT
This communication highlights the development of a nicotinamide series of histone deacetylase inhibitors within the benzamide structural class. Extensive exploration around the nicotinamide core led to the discovery of a class I selective HDAC inhibitor that possesses excellent intrinsic and cell-based potency, acceptable ancillary pharmacology, favorable pharmacokinetics, sustained pharmacodynamics in vitro, and achieves in vivo efficacy in an HCT116 xenograft model.
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Bases de datos:
MEDLINE
Asunto principal:
Inhibidores Enzimáticos
/
Inhibidores de Histona Desacetilasas
/
6-Aminonicotinamida
Tipo de estudio:
Prognostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Estados Unidos