Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).
Bioorg Med Chem Lett
; 18(6): 1859-63, 2008 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-18304810
ABSTRACT
An HTS screening campaign identified a series of low molecular weight phenols that showed excellent selectivity (>100-fold) for HDAC1/HDAC2 over other Class I and Class II HDACs. Evolution and optimization of this HTS hit series provided HDAC1-selective (SHI-1) compounds with excellent anti-proliferative activity and improved physical properties. Dose-dependent efficacy in a mouse HCT116 xenograft model was demonstrated with a phenylglycine SHI-1 analog.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fenilalanina
/
Neoplasias do Colo
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Proliferação de Células
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Inibidores Enzimáticos
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Inibidores de Histona Desacetilases
/
Glicina
Limite:
Animals
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Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2008
Tipo de documento:
Article