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Studies on the syntheses of heterocyclic compounds. 845. Studies on the synthesis of chemotherapeutics. 10. Synthesis and antitumor activity of N-acyl-and N-( …

T Kametani, K Kigasawa, M Hiiragi…

文献索引:Kametani, Tetsuji; Kigasawa, Kazuo; Hiiragi, Mineharu; Wakisaka, Kikuo; Haga, Seiji; et al. Journal of Medicinal Chemistry, 1980 , vol. 23, # 12 p. 1324 - 1329

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被引用次数: 59

摘要

A number of N-acyl and N-(alkoxycarbonyl)-5-fluorouracil derivatives possessing, for example, benzoyl, o-toluyl, acetyl, propionyl, heptanoyl, ethoxycarbonyl, phenoxycarbonyl, and benzyloxycarbonyl groups as N1 and/or N3 substituents were synthesized, and their antitumor activities were evaluated. The synthesis was achieved by a direct and two-step acylation of 5-fluorouracil (1) and by selective N1-deacetylation of Nl-acetyl-N3-substitukd ...