Synthesis And Biological Activity Of 5-flurouracil Derivatives Containing β-D-glucoside

Two series of novel 3 -D-glucoside-containing 5-flurouracil derivatives were synthesized. That is five N1-(2-furanidyl)- N3-(beta -D-acetylglucoside-l-yl)-5-fluro-uracil and five (beta-D-acetylglucoside-1-yl)- 5-fluoronracil-l-acetates. They were synthesized from corresponding 1-D-bromoacetylcarbohydrate with N1-(2-fiirnanidyl)-5-fluorouracil and 5-fluorouracil-l -acetic acid. The structures of these novel target compounds were confirmed by elemental analysis, IR, 1H NMR, MS respectively.The structures of the title compounds are as follows respectively, The preliminary anti-cancer activities tests of MI the two series targetcompounds were all finished at Institute of Materia Medicine in Chinese Academy of Medical Sciences. It is found that those compounds have better inhibitory activities against Bel-7402 (lung cancer cell) and HCT-8(colon cancer cell) than A-549(liver cancer cell) and Ib has the best inhibitory activity among the compounds.