[Synthesis and anticancer activity of norcantharidin-galactose derivatives].
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.
School of Pharmacy, Soochow University, Suzhou 215123, China.
Feng
F
Fan
Xiao-Fei
XF
Sun
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006528:Carcinoma, Hepatocellular / Q000473:pathology; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D005260:Female; D005690:Galactose / Q000737:chemistry*; D006801:Humans; D008113:Liver Neoplasms / Q000473:pathology; D008297:Male; D051379:Mice; D009368:Neoplasm Transplantation; D011355:Prodrugs / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D011355:Prodrugs; C069741:norcantharidin; D005690:Galactose