Antitumor activity of 1-alkylcarbamoyl derivatives of 5-fluorouracil against L1210 leukemia.

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Abstract
The relationship between chemical structure and antitumor activity of various 1-alkylcarbamoyl derivatives of 5-fluorouracil by parenteral and oral administrations was examined in the [mouse leukemia] L1210 system. By i.p. administration, when the carbon chain of the aliphatic derivatives was extended antitumor activity and toxicity to host animals were reduced gradually but ratios of reduction in activity and toxicity were different from each other. The butyl derivative showed the highest therapeutic ratio among the derivatives, though it was lower than the therapeutic ratio of 5-fluorouracil. By oral administration, antitumor activity and toxicity to host animals were decreased as the carbon chain of the aliphatic derivatives was extended. Therapeutic ratios of the compounds having even carbons in their side chain were greater than those of the adjoining compounds having odd carbons. Among them, 1-hexyl-carbamoyl-5-fluorouracil showed the highest therapeutic ratio. This compound was considered to be more suitable for treatment by oral administration than 5-fluorouracil, though the latter compound was superior than the former by parenteral administration.