Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
Bioorg Med Chem
; 23(24): 7597-606, 2015 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-26613635
ABSTRACT
The combination of antiestrogens and histone deacetylase inhibitors (HDACi) has been found to be antiproliferative in breast cancer models. We designed and synthesized hybrid structures which combined structural features of the pure antiestrogen ICI-164,384 and HDACi's SAHA and entinostat in a single bifunctional molecule. The hybrids retained antiestrogenic and HDACi activity and, in the case of benzamide hybrids, were selective for Class I HDAC3 over Class II HDAC6. The hybrids possessed low micromolar to high nanomolar activity against both ER+ MCF-7 and ER- MDA-MB-231 breast cancer cell models.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Mama
/
Moduladores de Receptor Estrogênico
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Inibidores de Histona Desacetilases
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Antineoplásicos
Limite:
Female
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Canadá