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

Acta Chimica Sinica ›› 2002, Vol. 60 ›› Issue (4): 720-724. Previous Articles Next Articles

Original Articles

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

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

National Laboratory of Applied Organic Chemistry, Lanzhou University,Lanzhou(730000)

Published:2002-04-15

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).

Key words: fluorouracil, podophyllotoxin, ANTICARCINOGEN, PROTEASE

CLC Number:

O621

Cite this article

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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新的4’-去甲表鬼臼衍生物的合成及其抗癌活性

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

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