Studies on Antitumor Agents. VI. Syntheses and Antitumor Activities of Acyl Derivatives of 2'-Deoxy-5-trifluoromethyluridine(Medicinal Chemistry,Chemical)
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- 山下 純一
- Kodama Institute, Taiho Pharmaceutical Co., Ltd.
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- 武田 節夫
- Tokushima Institute, Taiho Pharmaceutical Co., Ltd.
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- 松本 宏
- Tokushima Institute, Taiho Pharmaceutical Co., Ltd.
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- 寺田 忠史
- Kodama Institute, Taiho Pharmaceutical Co., Ltd.
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- 采見 憲男
- Tokushima Institute, Taiho Pharmaceutical Co., Ltd.
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- 安本 三治
- Kodama Institute, Taiho Pharmaceutical Co., Ltd.
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Various O-acyl and N-acyl derivatives of 2'-deoxy-5-trifluoromethyluridine (F_3Thd) were synthesized; namely 5'-O-acyl, 3',5'-di-O-acyl, N^3-acyl, 3',5'-di-O-acetyl-N^3-acyl, 3',5'-di-O-carbamoyl and 3',5'-di-O-ethoxycarbonyl compounds. 5'-O-Acyl derivatives of 2'-deoxy-5-trifluoromethylcytidine were also synthesized. The antitumor activities of these compounds against sarcoma 180 were examined by oral administration to mice. Among the 5'- and 3',5'-diester compounds with aliphatic acids, the 5'-O-hexanoyl compound showed the highest activity. Full protection of the sugar moiety with aroyl or carbamoyl groups considerably decreased the activities, and those of the 3',5'-di-O-m-fluorobenzoyl and 3',5'-di-O-butylcarbamoyl compounds were the smallest. N^3-Benzoyl compounds were slightly more effective than F_3Thd but none of them showed higher activity than the effective O-acyl compounds. In the case of 5'-O-acylates of 2'-deoxy-5-trifluoroniethylcytidine, the 5'-O-benzoyl compound showed the highest activity.
収録刊行物
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- Chemical & pharmaceutical bulletin
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Chemical & pharmaceutical bulletin 35 (5), 2090-2094, 1987-05-25
公益社団法人日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1573105977139626240
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- NII論文ID
- 110006281165
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- NII書誌ID
- AA00602100
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- ISSN
- 00092363
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- 本文言語コード
- en
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- データソース種別
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- CiNii Articles