Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation / 药学学报
Acta Pharmaceutica Sinica
; (12): 354-363, 2012.
Artigo
em Inglês
| WPRIM (Pacífico Ocidental)
| ID: wpr-323036
Biblioteca responsável:
WPRO
ABSTRACT
Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.
Texto completo:
Disponível
Base de dados:
WPRIM (Pacífico Ocidental)
Assunto principal:
Patologia
/
Farmacologia
/
Relação Estrutura-Atividade
/
Desenho de Fármacos
/
Estrutura Molecular
/
Química
/
Apoptose
/
Carcinoma Pulmonar de Células não Pequenas
/
Concentração Inibidora 50
/
Linhagem Celular Tumoral
Limite:
Humanos
Idioma:
Inglês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Artigo