Abstract
N(3)-Hydroxyethyltegafur (3) was synthesized in 91.0% yield under a new condition. A series of novel fatty acid esters of 3 were synthesized. These fatty acid-nucleoside conjugates have shown cytotoxicities against Ec9706 cells and A549 cells, and the structure activity relationship was discussed.
MeSH terms
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Antimetabolites, Antineoplastic / chemical synthesis*
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Antimetabolites, Antineoplastic / pharmacology*
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Esters / chemical synthesis
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Esters / pharmacology
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Fatty Acids / chemical synthesis*
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Fatty Acids / pharmacology*
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Humans
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Nucleosides / chemical synthesis*
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Nucleosides / pharmacology*
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Spectrometry, Mass, Electrospray Ionization
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Structure-Activity Relationship
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Tegafur / analogs & derivatives*
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Tegafur / chemical synthesis*
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Tegafur / pharmacology
Substances
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Antimetabolites, Antineoplastic
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Antineoplastic Agents
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Esters
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Fatty Acids
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Nucleosides
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Tegafur