Synthesis and antitumor activity of chitosan carrying 5-fluorouracils

摘要: In order to provide a polymeric drug of 5-fluorouracil (5FU) with reduced side-effects, having affinity for tumor cells and exhibiting high antitumor activity, four kinds chitosan derivatives were synthesized carrying 5FUs through some spacers via ether, amide, ester, or carbamoyl bonds. The release behaviors 5FU residues studied in vitro at 37°C various aqueous media. activity was tested against p-388 lymphocytic leukemia female CDF1 mice vivo by intraperitoneal injection the drugs followed (i. p./i. p.). Chitosan fixing 2-position hexamethylene spacer linkages (9) exhibits higher effect respect prolongation life than free 5FU. chitosan-5FU conjugates obtained do not display acute toxicity dose range.