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化学学报
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化学学报 ›› 2002, Vol. 60 ›› Issue (4): 720-724. 上一篇    下一篇

研究论文

新的4’-去甲表鬼臼衍生物的合成及其抗癌活性

张辅民;田瑄   

  1. 兰州大学,兰州(730000)
  • 发布日期:2002-04-15

Synthesis and Anti-cancer Activity of Novel Derivatives of 4'- Demethylepipodophyllotoxin

Zhang Fumin;Tian Xuan   

  1. National Laboratory of Applied Organic Chemistry, Lanzhou University,Lanzhou(730000)
  • Published:2002-04-15

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530

被引次数

2

根据鬼臼毒衍生物和5-氟尿嘧啶的抗癌机理和构效关系，合成了7个新的4β- 5-氟尿嘧啶取代-4’-去甲表鬼鬼臼毒衍生物。在抑制金属基质蛋白酶I和胶原酶I 活性测试中，化合物2.4和2.6的抑制活性比鬼臼乙叉甙（VP-16）和5-氟尿嘧啶（ 5-Fu）强的3倍和5倍，在治疗癌细胞转移方面值得进一步探讨。

关键词: 氟尿嘧啶, 鬼臼毒素, 抗癌药, 蛋白酶

According to the structure-activity relationship of podophyllotoxin derivatives, along with the different anti-cancer mechanism between demethylepipodophyllotoxin and 5-fluorouracil, seven novel 4β-5- fluorouracil substituted 4'-demethylepipodophyllotoxin derivatives were synthesized and evaluated as inhibitors of stromelysin-1 as well as collagenase-1. Among them, compounds 2.4 and 2.6 exhibited superior inhibitor activity against stromelysin-1 than that of prototype drugs, etoposide and 5-fluorouracil (inhibitory ratio were 80.2, 80.0, 25.5 and 15.8 for compounds 2.4, 2.6, etoposide and 5-Fu, respectively).

Key words: fluorouracil, podophyllotoxin, ANTICARCINOGEN, PROTEASE

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