Syntheses and Biological Activities of N^1-(2-Formylethyl)-5-fluorouracil and Related Compounds
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概要
- 論文の詳細を見る
Derivatives of 5-fluorouracil (5-FU) substituted at the N-1 position were synthesized in order to investigate their enzymatic conversion to N^1-(2-formylethyl)-5-FU, which is expected to give 5-FU with concomitant release of acrolein. Proton nuclear magnetic resonance spectroscopic studies of authentic N^1-(2-formylethyl)-5-FU suggested that the compound exists in an equilibrium mixture of free aldehyde and cyclic hemiacetal forms. Spontaneous liberation of 5-FU from N^1-(2-formylethyl)-5-FU at neutral pH was demonstrated by thin-layer chromatography using both the authentic compound and N^1-(3-aminopropyl)-5-FU after treatment with amine oxidase, but the release of 5-FU seemed to be limited. Cytotoxicity was observed with N^1-(2-formylethyl)-5-FU and N^1-(3-aminopropyl)-5-FU, but none of the derivatives of 5-FU presently prepared showed a positive effect on P388 leukemia inoculated into mice.
- 公益社団法人日本薬学会の論文
- 1985-06-25
著者
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岡田 正志
Tokyo Biochemical Research Institute
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松永 功
Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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岡田 正志
(財)東京生化学研究会
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松永 功
New Drug Research Laboratories Chugai Pharmaceutical Co. Ltd.
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越智 清成
Exploratory Research Laboratories, Chugai Pharmaceutical Co., Ltd.,
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越智 清成
Exploratory Research Laboratories Chugai Pharmaceutical Co. Ltd.
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松永 功
New Drug Research Laboratories, Chugai Pharmaceutical Co., Ltd.,
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