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5-Fluorouracil derivatives. XVII. Synthesis and antitumor activity of 5'-O-acyl-5-fluorouridines.
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1989
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Bioorganic ChemistryAntitumor ActivityChemoprevention StrategyPharmacotherapyPharmaceutical ChemistryMedicinal ChemistryAnti-cancer AgentL-1210 LeukemiaDerivativesBiochemistry5-Fluorouracil DerivativesFluorous SynthesisDrug DevelopmentPharmacologyNatural SciencesMedicineDerivative (Chemistry)Active DerivativesDrug Discovery
With the aim of diminishing the toxicity of 5-fluorouridine (1) and obtaining biologically active derivatives of 1, various kinds of 5'-O-acyl-5-fluorouridines 2 were synthesized. The antitumor activity of the compounds against L-1210 leukemia in mice was examined. The 5'-O-heptanoyl derivative 2h showed the highest antitumor activity.