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Inhibition of Uridine Ribonucleotide Synthesis by 5-Halogenated-2′-deoxyuridine Analogues

Abstract

PREVIOUS in vitro research1 with the halogenated analogues of orotic acid demonstrated the following basic experimental facts: First, to inhibit the conversion of orotic acid to the uridine nucleotides it was necessary for a drug to be a 5-substituted analogue of orotic acid. For example, it was found that 5-fluoro-orotic acid would inhibit orotic acid conversion, but that 5-fluoro uracil would not. Second, the order of activity of the 5 halogenated orotic acid analogues was fluorine > chlorine > bromine, and the 5-iodo compounds showed little or no activity.

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References

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STONE, J. Inhibition of Uridine Ribonucleotide Synthesis by 5-Halogenated-2′-deoxyuridine Analogues. Nature 204, 190–191 (1964). https://doi.org/10.1038/204190a0

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