高等学校化学学报

高等学校化学学报 ›› 2000, Vol. 21 ›› Issue (9): 1410.

• 研究简报 • 上一篇    下一篇

N3-羟烷基替加氟制备方法改良及其环甘油磷脂缀合物的合成与抗肿瘤活性

许新华, 陈焕明, 陈茹玉   

  1. 南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 天津 300071
  • 收稿日期:1999-11-08 出版日期:2000-09-24 发布日期:2000-09-24
  • 通讯作者: 陈茹玉(1919年出生),女,教授,博士生导师,中国科学院院士,主要从事药物和农药化学研究.
  • 基金资助:

    国家自然科学基金(批准号:29772018);国家教育部高等学校重点实验室基金资助

Improvement Preparation Method of N3-(Hydroxyalkyl) Tagefur and Synthesis and Activity of Its Cyclic Glycerophospholipid Conjugate

XU Xin-Hua, CHEN Huan-Ming, CHEN Ru-Yu   

  1. Institute of Elemento-Organic Chemistry, The State Key Laboratory of Elemento-organic Chemistry, Nankai University, Tianjin 300071, China
  • Received:1999-11-08 Online:2000-09-24 Published:2000-09-24

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关键词: 环甘油磷脂, 缀合物, 抗癌活性, 替加氟

Abstract: N1-(2-Fursnidyl)-5-fluorouracil reacted with multimethylenes chlorohydrin in the presence of NaHCO3 in acetonitrile at 80 ℃ to give N1-(2-furanidyl)-N3-(hydroxyalkyl)-5-fulorouracils in a high yield (≥93%). Their cyclic glycerophospholipid conjugates were synthesized and had a good activity against the man urinary bladder cancer cell in vitro.

Key words: Cyclic glycerophospholipid, Conjugates, Antitumor activity, Tagefur

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