- 著者
- SHOICHIRO OZAKI TOSHIO NAGASE HIROFUMI TAMAI HARUKI MORI AKIO HOSHI MASAAKI IIGO
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.9, pp.3894-3897, 1987-09-25 (Released:2009-10-19)
- 参考文献数
- 11
- 被引用文献数
- 8 9
For the purpose of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, alkylthiomethyl, alkylsulfinylmethyl, alkylsulfonylmethyl, and acylthiomethyl groups were introduced at the 1- and 3-positions of 1. The antitumor activity of these synthetic compounds was tested against L1210 leukemia in mice. 1-Alkylthiomethyl-5-fluorouracils showed weak antitumor activity at a high dose (300 mg/kg).
1 0 0 0 OA A Facile Method for Synthesis of N-Acyloxymethyl-5-fluorouracils, as a Class of Antitumor Agents
- 著者
- SUHAIL AHMAD SHOICHIRO OZAKI TOSHIO NAGASE MASAAKI IIGO REIKO TOKUZEN AKIO HOSHI
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.10, pp.4137-4143, 1987-10-25 (Released:2009-10-19)
- 参考文献数
- 15
- 被引用文献数
- 23 24
Antitumor-active derivatives of 5-fluorouracil were prepared via a new method by introducing an acyloxymethyl group at the 1-, 3-, or 1, 3-position (s). These derivatives were obtained by condensing 1, 3-bis (hydroxymethyl) -5-fluorouracil with various short-/long-chain carboxylic acids or their derivatives, in the presence of dicyclohexylcarbodiimide and a catalytic amount of N, N-dimethylaminopyridine. Some of the derivatives showed strong antitumor activity against the leukemia L1210 system when administered orally.