1.
Bioorg Med Chem Lett
; 13(19): 3331-5, 2003 Oct 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12951120
RESUMO
Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.
Assuntos
Amidas/química , Amidas/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores de Histona Desacetilases , Animais , Linhagem Celular Tumoral , Histona Desacetilases/metabolismo , Humanos , Camundongos , Ensaios Antitumorais Modelo de Xenoenxerto/métodos
2.
Bioorg Med Chem Lett
; 12(23): 3443-7, 2002 Dec 02.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12419380
RESUMO
Trifluoromethyl ketones were found to be inhibitors of histone deacetylases (HDACs). Optimization of this series led to the identification of submicromolar inhibitors such as 20 that demonstrated antiproliferative effects against the HT1080 and MDA 435 cell lines.
