A cyclodextrin-capped histone deacetylase inhibitor.
Bioorg Med Chem Lett
; 23(11): 3346-8, 2013 Jun 01.
Article
en 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
Bases de datos:
MEDLINE
Asunto principal:
Proteínas Represoras
/
Beta-Ciclodextrinas
/
Inhibidores de Histona Desacetilasas
/
Histona Desacetilasas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article
País de afiliación:
Reino Unido