Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors.
Bioorg Med Chem Lett
; 18(3): 1067-71, 2008 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-18160287
ABSTRACT
Inhibition of histone deacetylases (HDAC) is emerging as a new strategy in human cancer therapy. The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides is presented herein. From the different series bearing a six-membered heteroaromatic ring studied, the s-triazine series showed the best HDAC1 enzyme and in vitro anti-proliferative activities with IC(50) values below micromolar range. Some of these compounds can also significantly reduce tumor growth in human tumor xenograft models in mice.
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Triazinas
/
Benzamidas
/
Inibidores Enzimáticos
/
Inibidores de Histona Desacetilases
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Canadá