Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett
; 18(23): 6078-82, 2008 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-18952417
ABSTRACT
5-(Trifluoroacetyl)thiophene-2-carboxamides were found to be potent and selective class II HDAC inhibitors. This paper describes their further development and the investigation on the cause for the lack of cell-based activity. A rapid screening assay was set up which enabled the identification of more metabolic stable compounds as potent and selective class II HDAC inhibitors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tiofenos
/
Inibidores de Histona Desacetilases
/
Amidas
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article