Abstract
In an attempt to improve the effectiveness of action of 5-fluoro-2'-deoxyuridine (FUdR), various kinds of O-alkylated water-soluble analogues were synthesized. Antitumor activities against sarcoma 180 (solid) were also evaluated. Some compounds exhibited potent activities. In particular, 3'-O-p-chlorobenzyl-3-N-aminoacyloxy-methylester derivatives were effective over a very wide range of dose and gave extremely large therapeutic ratios compared with known 5-fluorouracil (5-FU) derivations.
MeSH terms
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Animals
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Antimetabolites, Antineoplastic / chemical synthesis*
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Antimetabolites, Antineoplastic / pharmacokinetics
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Antimetabolites, Antineoplastic / pharmacology
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Chemical Phenomena
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Chemistry, Physical
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Deoxyuridine / analogs & derivatives
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Deoxyuridine / chemical synthesis*
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Deoxyuridine / pharmacokinetics
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Deoxyuridine / pharmacology
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Female
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Floxuridine / analogs & derivatives*
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Floxuridine / chemical synthesis
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Floxuridine / pharmacology
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Mice
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Mice, Inbred ICR
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Sarcoma 180 / drug therapy
Substances
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Antimetabolites, Antineoplastic
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Floxuridine
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Deoxyuridine