Studies on antitumor agents. IV. Syntheses and antitumor activities of compounds related to 1-(tetrahydro-2-furanyl)-5-fluorouracil metabolites.

• 上田 修一

• 武田 節夫

• 山脇 一郎

• 山下 純一

• 安本 三治

• 橋本 貞夫

抄録

A hydroxylated metabolite of 1-(tetrahydro-2-furanyl)-5-fluorouracil (FT), 1-(trans-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (trans-3'-OH-FT, VIII) and its isomer, 1-(cis-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (cis-3'-OH-FT, VI), were synthesized and isolated at high purity. As compounds related to FT metabolites, 2, 3'-anhydro-1-(cis-3-hydroxytetrahydro-2-furanyl)-5-fluorouracil (2, 3'-anhydro-FT, V), 1-(2, 5-dihydro-2-furanyl)-5-fluorouracil (3', 4'-dehydro-FT, XII) and 1-(5-acetoxytetrahydro-2-furanyl)-5-fluorouracil (5'-AcO-FT, XI) were also synthesized. The antitumor activities of these compounds against sarcoma 180 and L 1210 were examined. The activities of cis-3'-OH-FT (VI) and 2, 3'-anhydro-FT (V) were found to be lower than that of FT. The activity of 5'-AcO-FT (XI) was the same as that of FT. 3', 4'-Dehydro-FT (XII) showed much greater activity than FT.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 30 (1), 125-131, 1982

  公益社団法人 日本薬学会

キーワード

• NMR shift reagent

詳細情報

• CRID: 1390001204164686720
• NII論文ID: 110003634068
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.30.125
• ISSN: 13475223
• ISSN: 00092363
• PubMed: 7083401
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/30/1/30_1_125/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1982209960
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可