Antitumor activity of metabolites of 1-hexylcarbamoyl-5-fluorouracil and related compounds against L1210 leukemia in vivo and L5178Y lymphoma cells in vitro.

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Abstract
Antitumor activity of metabolites of 1-hexylcarbamoyl-5-fluorouracil (HCFU) and related compounds was examined in vivo and in vitro. Carboxypentyl and carboxypropyl carbamoyl derivatives of 5-fluorouracil (FU) were moderately active against [mouse leukemia] L1210 cells by oral administration, but less active by i.p. administration. 5-Hydroxy- and 5-oxo-hexyl carbamoyl derivatives of FU were markedly or moderately active against the leukemia by oral and i.p. administrations. Therapeutic ratios for the metabolites were less than that for HCFU by oral and i.p. administrations. Metabolites of HCFU had growth inhibitory activity against [mouse lymphoma] L5178Y cells in vitro similar to alkylcarbamoyl derivatives of FU. Activity of metabolites was lower than that of FU, and higher than that of HCFU in vitro. HCFU is converted into FU through active intermediate metabolites in vivo.