Chemical Modification of an Antitumor Alkaloid, 20(S)-Camptothecin : Glycosides, Phosphates and Sulfates of 7-Ethyl 10-hydroxycamptothecin
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概要
- 論文の詳細を見る
Water-soluble derivatives having the lactone ring intact were synthesized starting from 7-ethyl-10-hydroxycamptothecin (1). Glycosides (2) of the phenolic hydroxyl group of 1 were obtained by reaction with acetylated α-bromosugars in acetone or aqueous acetone in the presence of potassium carbonate, followed by deprotection.Phosphates (3) were prepared by reaction of 1 with phosphoryl chloride in pyridine or with dibenzylchlorophosphoridate.Sulfates (4) were obtained by reaction of 1 with sulfur trioxide-pyridine complex in the presence of a tertiary amine.The organic ammonium salts of monophosphate (3p) and sulfates (4a and 4b) showed significant activity against L1210 in vivo.
- 公益社団法人日本薬学会の論文
- 1992-01-25
著者
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宮坂 貞
School of Pharmaceutical Sciences, Showa University
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八重樫 隆
Yakult Central Institute of Microbiological Research
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澤田 誠吾
Yakult Central Institute of Microbiological Research
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澤田 誠吾
ヤクルト本社中央研究所
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横倉 輝男
ヤクルト中央研究所
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横倉 輝男
Yakult Central Institute for Microbiological Research
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沢田 誠吾
Yakult Central Institute for Microbiological Research
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古田 富雄
Yakult Central Institute for Microbiological Research
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野方 健一郎
Yakult Institute for Microbiological Research
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横倉 輝雄
Yakult Institute for Microbiological Research
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Sawada S
Yakult Central Institute Of Microbiological Research
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宮坂 貞
School Of Pharmaceutical Sciences Showa University
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野方 健一郎
Yakult Central Institute For Microbiological Research
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横倉 輝男
ヤクルト本社 中研
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横倉 輝男
Yakult Central Institute
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