Antitumor Activity of 1-Alkylcarbamoyl Derivatives of 5-Fluorouracil against L1210 Leukemia

概要

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Relationship between chemical structure and antitumor activity of various 1-alkylcarbamoyl derivatives of 5-fluorouracil by parenteral and oral administrations was examined in L1210 system. By intraperitoneal administration, in aliphatic derivatives, when carbon chain extended stepwisely, both antitumor activity and toxicity to host animals were reduced gradually, but ratios of reduction in activity and toxicity were different each other. tert-Butyl derivative showed the highest therapeutic ratio among the derivatives. However, it was lower than the therapeutic ratio of 5-fluorouracil. On the other hand, by oral administration, antitumor activity and toxicity to host animals were decreased along the extention of carbon chain in aliphatic derivatives and 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-hexylcarbamoyl-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.
社団法人日本薬学会の論文
1978-01-25