Abstract
A series of water soluble N(1)- and C(6)-substituted uracil pyridinium compounds were prepared as potential inhibitors of thymidine phosphorylase (TP). The C(6)-uracil substituted derivatives were the most active. 1-[(5-Chloro-2,4-dihydroxypyrimidin-6-yl)methyl]pyridinium chloride, was identified as the best inhibitor being 5-fold more potent than the known inhibitor, 6-amino-5-bromouracil.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Escherichia coli / enzymology
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Inhibitory Concentration 50
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Neovascularization, Pathologic / drug therapy
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Pyridinium Compounds / chemical synthesis*
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Pyridinium Compounds / pharmacology
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Solubility
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Structure-Activity Relationship
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Thymidine Phosphorylase / antagonists & inhibitors*
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Uracil / analogs & derivatives
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Uracil / chemical synthesis*
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Uracil / pharmacology
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Pyridinium Compounds
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Uracil
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Thymidine Phosphorylase