Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
Bioorg Med Chem Lett
; 20(22): 6657-60, 2010 Nov 15.
Article
em En
| MEDLINE
| ID: mdl-20884208
ABSTRACT
Inhibition of histone deacetylase activity represents a promising new modality in the treatment of a number of cancers. A novel HDAC series demonstrating inhibitory activity in cell proliferation assays is described. Optimisation based on the introduction of basic amine linkers to effect good drug distribution to tumour led to the identification of a compound with oral activity in a human colon cancer xenograft study associated with increased histone H3 acetylation in tumour tissue.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Desenho de Fármacos
/
Inibidores de Histona Desacetilases
/
Ácidos Hidroxâmicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article