Synthesis and cytotoxic activity of novel derivatives of 4′-demethylepipodophyllotoxin
Synthesis and cytotoxic activity of novel derivatives of 4′-demethylepipodophyllotoxin
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DOI：
10.1016/j.bmcl.2004.07.094
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发表时间：
2004-10-18
影响因子：
2.7
通讯作者：
Tu, YQ
中科院分区：
文献类型：
--
作者：
Chen, SW;Xuan, T;Tu, YQ
合成了9个4 β-N-取代-5-FU-4 ′-去甲基表鬼臼毒素衍生物，并对其抗肿瘤活性进行了评价。所有目标化合物对HL-60和A-549的体外细胞毒活性均高于VP-16和5-FU。其中，4 β-N-取代苯丙氨酸5-Fu戊酯-4 ′-去甲基表鬼臼毒素（9 g）对HL-60和A-549细胞的杀伤活性最强（IC_（50）分别为0.04和0.05）。
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