| 新的4’-去甲表鬼臼衍生物的合成及其抗癌活性 |
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| 引用本文： | 张辅民,田瑄.新的4’-去甲表鬼臼衍生物的合成及其抗癌活性[J].化学学报,2002,60(4):720-724. |
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| 作者姓名： | 张辅民 田瑄 |
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| 作者单位： | 兰州大学,兰州(730000) |
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| 基金项目： | 甘肃省自然科学基金(ZS001-A23-052-Y)资助项目. |
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| 摘 要： | 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。
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| 关 键 词： | 氟尿嘧啶 鬼臼毒素 抗癌药 蛋白酶 |
| 修稿时间： | 2001年7月4日 |
Synthesis and Anti-cancer Activity of Novel Derivatives of 4'- Demethylepipodophyllotoxin |
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| Zhang Fumin,Tian Xuan.Synthesis and Anti-cancer Activity of Novel Derivatives of 4'- Demethylepipodophyllotoxin[J].Acta Chimica Sinica,2002,60(4):720-724. |
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| Authors: | Zhang Fumin Tian Xuan |
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| Institution: | National Laboratory of Applied Organic Chemistry, Lanzhou University,Lanzhou(730000) |
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| Abstract: | 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). |
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| Keywords: | fluorouracil podophyllotoxin ANTICARCINOGEN PROTEASE |
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