Studies on Antitumor Agents. IV. Syntheses and Antitumor Activities of Compounds related to 1-(Tetrahydro-2-furanyl)-5-fluorouracil Metabolites
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概要
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A hydroxylated metabolite of 1-(tetrahydro-2-furanyl)-5-fluorouracil (FT), 1-(trans-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (trans-3'-OH-FT, VIII) and its isomer, 1-(cis-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (cis-3'-OH-FT, VI), were synthesized and isolated at high purity. As compounds related to FT metabolites, 2,3'-anhydro-1-(cis-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (2,3'-anhydro-FT, V), 1-(2,5-dihydro-2-furanyl)-5-fluorouracil (3', 4'-dehydro-FT, XII) and 1-(5-acetoxytetrahydro-2-furanyl)-5-fluorouracil (5'-AcO-FT, XI) were also synthesized. The antitumor activities of these compounds against sarcoma 180 and L 1210 were examined. The activities of cis-3'-OH-FT (VI) and 2,3'-anhydro-FT (V) were found to be lower than that of FT. The activity of 5'-AcO-FT (XI) was the same as that of FT. 3', 4'-Dehydro-FT (XII) showed much greater activity than FT.
- 社団法人日本薬学会の論文
- 1982-01-25
著者
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山下 純一
Hanno Research Center, Taiho Pharmaceutical Co., Ltd.,
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武田 節夫
Tokushima Institute, Taiho Pharmaceutical Co., Ltd.,
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武田 節夫
Research Institute, Taiho Pharmaceutical Co., Ltd.,
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山下 純一
Hanno Research Center Taiho Pharmaceutical Co. Ltd.
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安本 三治
Kodama Institute, Taiho Pharmaceutical Co., Ltd.,
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山下 純一
Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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安本 三治
Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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橋本 貞夫
Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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上田 修一
Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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山脇 一郎
Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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安本 三治
Kodama Institute Taiho Pharmaceutical Co. Ltd.
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武田 節夫
Tokushima Institute Taiho Pharmaceutical Co. Ltd.
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上田 修一
Research Laboratory Taiho Pharmaceutical Co. Ltd.
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橋本 貞夫
Research Institute Taiho Pharmaceutical Co. Ltd.
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山脇 一郎
Tokushima Research Center Pharmacokinetics Research Lab. Taiho Pharmaceutical Co. Ltd.
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