Synthesis and anticancer activity of norcantharidin-galactose derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 157-161, 2008.
Artigo
em Chinês
| WPRIM
| ID: wpr-268153
ABSTRACT
To design and synthesize the hepatic targeting anticancer prodrug with norcantharidin (NCTD-Gal) conjugating structure, galactosylated NCTD derivatives were synthesized from NCTD analogues modified by a series of amino acids via acylation, hydrolysis, glycosylation and deacetylation. Seven new compounds were synthesized as beta-O-glycosides and characterized by IR, MS, NMR and element analysis. The compound 4a was chosen for the inchoate antitumor experiments on mice. The result showed that the antitumor inhibition rate of 4a groups with medium and high dose are clearly higher than that of NCTD group, which suggests that anticancer effect of NCTD is improved at a certain degree by galactosylation.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Patologia
/
Farmacologia
/
Pró-Fármacos
/
Química
/
Sistemas de Liberação de Medicamentos
/
Carcinoma Hepatocelular
/
Compostos Bicíclicos Heterocíclicos com Pontes
/
Linhagem Celular Tumoral
/
Galactose
/
Neoplasias Hepáticas
Limite:
Animais
/
Feminino
/
Humanos
/
Masculino
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2008
Tipo de documento:
Artigo
Similares
MEDLINE
...
LILACS
LIS