Synthesis and cytotoxic activity of novel derivatives of 4′-demethylepipodophyllotoxin

被引：51

作者：

Chen, SW

Xuan, T ^{[1
]}

Tu, YQ

机构：

[1] Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China

[2] Lanzhou Univ, Dept Chem, Lanzhou 730000, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

基金：

中国国家自然科学基金;

关键词：

podophyllotoxin; 5-FU; amino acid; antitumor drugs;

D O I：

10.1016/j.bmcl.2004.07.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Nine novel 4beta-N-substituted-5-FU-4'-demethylepipodophyllotoxin derivatives were synthesized and evaluated as potential antitumor agents. All of the target compounds showed more significant cytotoxic activity against HL-60 and A-549 in vitro than VP-16 and 5-FU. Among them, 4beta-N-substituted-phenylalanine 5-Fu pentyl ester-4'-demethylepipodophyllotoxin (9g) was found to exhibit most potent cytotoxic activity against HL-60 and A-549 cell (IC50 is 0.04 and <0.01 muM, respectively). (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：5063 / 5066

页数：4

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