Chemical Modification of an Antitumor Alkaloid Camprothecin : Synthesis and Antitumor Activity of 7-C-Substituted Camptothecins
スポンサーリンク
概要
- 論文の詳細を見る
A radical substitution reaction of 20(S)-camptothecin (1) with methanol furnished 7-hydroxymethylcamptothecin (2). Reaction of 1 with primary alcohols higher than methanol gave 7-alkylcamptothecins (4), of which alkyl groups were one carbon less than the alcohols used and also 7-hydroxyalkylcamptothecins (5). For the preparation of 7-alkylcamptothecin (4), aldehydes were used as a radical source and several alkylated derivatives were synthesized. 7-Acyloxymethyl derivatives (6), 7-carbaldehyde (7), iminomethyl derivatives (10), acid (11), esters (12) and amides (13) were synthesized starting from 2. 7-Ethyl-(4b) and 7-propylcamptothecin (4c), acyloxymethyl compounds 6a, 6c and ethyl ester (12b) exhibited higher antitumor activity than 1 against L1210 in mice.
- 公益社団法人日本薬学会の論文
- 1991-10-25
著者
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宮坂 貞
School of Pharmaceutical Sciences, Showa University
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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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