Synthesis and antitumor activity of 6-O-carboxymethyl chitin fixing 5-fluorouracils through pentamethylene, monomethylene spacer groups via amide, ester bonds.
In order to provide the water-soluble and biodegradable macromolecular prodrug of 5-fluorouracil (5FU), the fixation of 5FUs to 6-O-carboxymethyl chitin(CM-chitin) through pentamethylene, monomethylene spacer groups via amide, ester bonds was carried out. The obtained CM-chitin/5FU conjugate showed the slow release of 5FU and exhibited remarkable antitumor activity against P388 lymphocytic leukemia in mice by intraperitoneal(i.p.) implantation/i.p. injection.
Ohya
Y
Y
Department of Applied Chemistry, Faculty of Engineering, Kansai University, Osaka, Japan.
Inosaka
K
K
Ouchi
T
T
D000818:Animals; D002686:Chitin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D005260:Female; D005472:Fluorouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use*; D007941:Leukemia P388 / Q000188:drug therapy*; D051379:Mice; D011355:Prodrugs / Q000138:chemical synthesis / Q000627:therapeutic use*
D011355:Prodrugs; D002686:Chitin; C075131:6-O-carboxymethylchitin-5-fluorouracil; C044872:O-(carboxymethyl)chitin; D005472:Fluorouracil