Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
Bioorg Med Chem Lett
; 24(23): 5450-4, 2014 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-25454270
ABSTRACT
Acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide are potent sub-type selective HDAC6 inhibitors. Constrained heterocyclic analogs based on 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine show further enhanced HDAC6 selectivity and inhibitory activity in cells. Homology models suggest that the heterocyclic spacer can more effectively access the wider catalytic channel of HDAC6 compared to other HDAC sub-types.
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Base de dados:
MEDLINE
Assunto principal:
Pirazinas
/
Inibidores de Histona Desacetilases
/
Ácidos Hidroxâmicos
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article