Synthesis and anticancer activity of norcantharidin-galactose derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 157-161, 2008.
Artículo
en Chino
| 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:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Patología
/
Farmacología
/
Profármacos
/
Química
/
Sistemas de Liberación de Medicamentos
/
Carcinoma Hepatocelular
/
Compuestos Bicíclicos Heterocíclicos con Puentes
/
Línea Celular Tumoral
/
Galactosa
/
Neoplasias Hepáticas
Límite:
Animales
/
Femenino
/
Humanos
/
Masculino
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2008
Tipo del documento:
Artículo
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