Activity of Esterase in the Hydrolysis of 3', 5'-Diesters of 5-Fluoro-2'-deoxyuridine in Relation to the Structure of the Diester Prodrugs
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概要
- 論文の詳細を見る
The activity of porcine liver esterase towards diesters of 5-fluoro-2'-deoxyuridine with saturated aliphatic acids including acetic, propionic, butyric, hexanoic, octanoic, decanoic and dodecanoic acids was investigated. The susceptibility of the 3', 5'-diesters increased as the acyl chain was lengthened up to octanoyl, but further increase in the acyl chain length resulted in a sharp decrease in the susceptibility. The susceptibility of 3'-and 5'-monoesters increased as the chain was lengthened to decanoyl and slightly decreased on going to dodecanoyl. These results suggest that the higher antitumor activity of longer alkyl chain diesters of 5-fluoro-2'-deoxyuridine is partly due to their slow rates of hydrolysis by non-specific esterase.
- 公益社団法人日本薬学会の論文
- 1985-01-25
著者
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南部 直樹
Faculty Of Pharmaceutical Sciences Hoshi University
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永井 恒司
星薬科大学 薬剤
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永井 恒司
Faculty of Pharmaceutical Sciences, Hoshi University
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鈴木 嘉樹
Bio-Medical Research Institute, Teijin Limited
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川口 健夫
Bio-Medical Research Institute, Teijin Limited
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中原 葉子
Faculty of Pharmaceutical Sciences, Hoshi University
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川口 健夫
Faculty Of Pharmaceutical Sciences Josai University
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鈴木 嘉樹
Faculty Of Pharmaceutical Sciences Hoshi University
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中原 葉子
Faculty Of Pharmaceutical Sciences Hoshi University
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