Study on N'hydroxyalkyl l-5-fluorouracils and α -5-fluorouracil-N'dicarboxylic acids

Abstract

N1-Hydroxyalkyl-5-fluorouracils, di-Et a-5-fluorouracil-N1-malonate, di-Me a-5 fluorouracil-N1-methylsuccinate, a-5-fluorouracil-N1-malonic acid and a-5-fluorouracil-N1-methylsuccinic acid were synthesized and structurally confirmed by 1H NMR, IR, UV and elemental anal. The antitumor activity of five 5-fluorouracil derivatives were tested against Ehrlich ascites carcinoma in mice and compared with that of 5-fluorouracil-N1-acetic acid and 5-fluorouracil-N1-propanoic acid. 5-Fluorouracil-N1-substituted dicarboxylic acids exhibited no antitumor activity. N1-Hydroxyethyl-5-fluorouracil and N1-hydroxypropyl-5-fluorouracil, with lower toxicity than 5-fluorouracil, showed an inhibition ratio of 52.40% and 67.32%, resp.

Key words: FLUOROURACILUM, FLUOROURACILUM, ESTERS, BROMINE COMPOUNDS, MALONIC ACID P, NMR SPECTROMETRY, ACETIC ACID P, INFRARED SPECTROPHOTOMETRY, BUTANEDIOIC ACID P, MALONIC ACID P

CLC Number:

O627
R914

Cite this article

ZHUO RENXI;FAN CHANGLIE;LIAO JUN;SONG QI. Study on N'hydroxyalkyl l-5-fluorouracils and α -5-fluorouracil-N'dicarboxylic acids[J]. Chin. J. Org. Chem., 1990, 10(6): 513-516.

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