Hydroxamates of para-aminobenzoic acid as selective inhibitors of HDAC8.
Bioorg Chem
; 57: 116-120, 2014 Dec.
Article
en En
| MEDLINE
| ID: mdl-25462986
ABSTRACT
A series of hydroxamates (4a-4l) were prepared from p-aminobenzoic acid to inhibit HDAC8. The idea is to substitute rigid aromatic ring in place of less rigid piperazine ring of hydroxamates reported earlier by our group. It is expected to increase potency retaining the selectivity. Result obtained suggested that the modifications carried out retained the selectivity towards HDAC8 isoform and increasing the potency in very few cases. Increase in potency is also associated with variation in cap aryl region. Two compounds (4f &4l) were found to inhibit HDAC8 at concentrations (IC50) less than 20µM.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Proteínas Represoras
/
Ácido 4-Aminobenzoico
/
Inhibidores de Histona Desacetilasas
/
Ácidos Hidroxámicos
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Bioorg Chem
Año:
2014
Tipo del documento:
Article
País de afiliación:
India