A cyclodextrin-capped histone deacetylase inhibitor.
Bioorg Med Chem Lett
; 23(11): 3346-8, 2013 Jun 01.
Article
em En
| MEDLINE
| ID: mdl-23591111
ABSTRACT
We have synthesized a ß-cyclodextrin (ßCD)-capped histone deacetylase (HDAC) inhibitor 3 containing an alkyl linker and a zinc-binding hydroxamic acid motif. Biological evaluation (HDAC inhibition studies) of 3 enabled us to establish the effect of replacing an aryl cap (in SAHA (vorinostat,)) 1 by a large saccharidic scaffold "cap". HDAC inhibition was observed for 3, to a lesser extent than SAHA, and rationalized by molecular docking into the active site of HDAC8. However, compound 3 displayed no cellular activity.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Proteínas Repressoras
/
Beta-Ciclodextrinas
/
Inibidores de Histona Desacetilases
/
Histona Desacetilases
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article