N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors.
Bioorg Med Chem Lett
; 17(24): 6729-33, 2007 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-17977726
ABSTRACT
A variety of N-(2-amino-phenyl)-4-(heteroarylmethyl)-benzamides were designed and synthesized. These compounds were shown to inhibit recombinant human HDAC1 with IC(50) values in the sub-micromolar range. In human cancer cells growing in culture these compounds induced hyperacetylation of histones, induced the expression of the tumor suppressor protein p21(WAF1/Cip1), and inhibited cellular proliferation. Certain compounds of this class also showed in vivo activity in various human tumor xenograft models in mice.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzamidas
/
Inibidores Enzimáticos
/
Inibidores de Histona Desacetilases
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article