1 0 0 0 OA 5-Fluorouracil Derivatives. IV. Synthesis of Antitumor-Active Acyloxyalkyl-5-fluorouracils
- 著者
- 尾崎 庄一郎 渡辺 裕 星子 知範 水野 晴雄 石川 勝敏 森 春樹
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.32, no.2, pp.733-738, 1984-02-25 (Released:2008-03-31)
- 参考文献数
- 16
- 被引用文献数
- 20 24
The toxicity and tumor affinity of 5-fluorouracil (1) have been modified by the introduction of acyloxyalkyl group (s) at the 1-, 3- or 1, 3-position (s) of 1. 1-Acyloxyalkyl-5-fluorouracil (3), 3-acyloxyalkyl-5-fluorouracil (4) and 1, 3-bis (acyloxyalkyl)-5-fluorouracil (5) were obtained by three methods : i) the reaction of α-chloroalkyl carboxylate (2) with 1, ii) the reaction of alkylidene diacylate with 2, 4-bis (trimethylsilyloxy)-5-fluoropyrimidine, iii) partial hydrolysis of 5. Compounds 3, 4 and 5 showed antitumor activity.
1 0 0 0 OA 5-Fluorouracil Dirivatives. XVII. : Synthesis and Antitumor Activity of 5'-O-Acyl-5-fluorouridines
- 著者
- 尾崎 庄一郎 秋山 隆彦 池 祥雅 森 春樹 星 昭夫
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.37, no.12, pp.3405-3408, 1989-12-25 (Released:2008-03-31)
- 参考文献数
- 13
- 被引用文献数
- 14 15
With the aim of diminishing the toxicity of 5-fluorouridine (1) and obtaining biologically active derivatives of 1, various kinds of 5'-O-acyl-8-fluorouridines 2 were synthesized. The antitumor activity of the compounds against L-1210 leukemia in mice was examined. The 5'-O-heptanoyl derivative 2h showed the highest antitumor activity.