Abstract
The 5'-phosphate (1) of the antiviral nucleoside 5-cyano-2'-deoxyuridine was synthesized and evaluated for inhibition of thymidylate synthetase purified from methotrexate-resistant Lactobacillus casei. Compound 1 was a potent competitive inhibitor with a K1 of 0.55 microns. Irreversible enzyme inhibition by this compound could not be detected.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Deoxyuracil Nucleotides / chemical synthesis*
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Deoxyuracil Nucleotides / pharmacology
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Lacticaseibacillus casei / enzymology
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Methyltransferases / antagonists & inhibitors*
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Nitriles / chemical synthesis
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Nitriles / pharmacology
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Structure-Activity Relationship
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Thymidylate Synthase / antagonists & inhibitors*
Substances
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5-cyano-2'-deoxyuridine 5'-phosphate
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Deoxyuracil Nucleotides
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Nitriles
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Methyltransferases
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Thymidylate Synthase