高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (S1): 228.

• Organic Synthesis Chemistry • 上一篇    下一篇

Synthesis of 1,2-Cyclic Monoacyl-rac-Glycerothio-phosphates of Cantharidin Analogs

ZHOU Zheng-Hong, CHEN Ru-Yu   

  1. Institute of Elemento-Oganic Chemistry, Nankai University, Tianjin 300071
  • 出版日期:1998-12-31 发布日期:1998-12-31
  • 基金资助:
    National Natural Science Foundation of China (Project 29572053)

Synthesis of 1,2-Cyclic Monoacyl-rac-Glycerothio-phosphates of Cantharidin Analogs

ZHOU Zheng-Hong, CHEN Ru-Yu   

  1. Institute of Elemento-Oganic Chemistry, Nankai University, Tianjin 300071
  • Online:1998-12-31 Published:1998-12-31
  • Supported by:
    National Natural Science Foundation of China (Project 29572053)

摘要: Mylabris, the dried body of the Chinese blister beetle, has been used as Chinese medicine for over 2000 years. Its active constituent, cantharidin, has anti tumor activities and causes leukocytosis. The synthesis of cyclic glycerophospholipid containing cantharidin analogs has so far not been reported in literature. The conjugates of this type are not only new prodrugs of cantharidin antitumor agents but also may generate two cytotoxic groups against different target sites inside a neoplastic cell. Such types of compounds may be of interest in chemistry, biochemistry and pharmacology. This paper deals with the synthesis of 1,2-cyclic monoacyl-rac-glycerothiophosphates of cantharidin analogs as new models of phospholipids.

Abstract: Mylabris, the dried body of the Chinese blister beetle, has been used as Chinese medicine for over 2000 years. Its active constituent, cantharidin, has anti tumor activities and causes leukocytosis. The synthesis of cyclic glycerophospholipid containing cantharidin analogs has so far not been reported in literature. The conjugates of this type are not only new prodrugs of cantharidin antitumor agents but also may generate two cytotoxic groups against different target sites inside a neoplastic cell. Such types of compounds may be of interest in chemistry, biochemistry and pharmacology. This paper deals with the synthesis of 1,2-cyclic monoacyl-rac-glycerothiophosphates of cantharidin analogs as new models of phospholipids.

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