Synthesis and anticancer activity of norcantharidin-galactose derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 157-161, 2008.
Article
Dans Chinois
| 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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Anatomopathologie
/
Pharmacologie
/
Promédicaments
/
Chimie
/
Systèmes de délivrance de médicaments
/
Carcinome hépatocellulaire
/
Composés hétérocycliques bicycliques
/
Lignée cellulaire tumorale
/
Galactose
/
Tumeurs du foie
Limites du sujet:
Animaux
/
Femelle
/
Humains
/
Mâle
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2008
Type:
Article
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