Study on N~1-Hydroxyalkyl-5-Fluorouracils and α-5-Fluorouracil-N~1-Dicarboxylic Acids

N~1-Hydroxyalkyl-5-fluorouracils, diethyl α-5-fluorouracil-N~1-malonate, dimethylα-5-fluorouracil-N~1-methylsuccinate, α-5-fluorouracil-N~1-malonic acid and α-5-fluorouracil-N~1-methylsuccinic acid were synthesized and structurally confirmed by ~1H NMR, IR, UVand elemental analysis. The antitumor activity of five 5-fluorouracil derivatives were testedagainst Ehrlish ascites carcinoma (EAC) in mice and compared with that of 5-fluorouracil-N~1-acetic acid and 5-fluorouracil-N~1-propanoic acid. 5-Fluorouracil-N~1-substituted dicarboxy-lic acids exhibited no antitumor activity. N~1-Hydroxyethyl-5-fluorouracil and N~1-hydroxy-propyl-5-fluorouracil, with lower toxicity than 5-fluorouracil, showed an inhibition ratio of52.40% and 67.32%, respectively.