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
em 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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Base de dados:
MEDLINE
Assunto principal:
Inibidores Enzimáticos
/
Inibidores de Histona Desacetilases
/
6-Aminonicotinamida
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article