尹述凡, 王志光, 马维勇, 陈秀华, 王天都, 张椿年. 4-O-卤代酰基-4′-去甲基表鬼臼毒素类似物的合成与抗肿瘤活性J. 药学学报, 1993, 28(10): 758-761.
引用本文: 尹述凡, 王志光, 马维勇, 陈秀华, 王天都, 张椿年. 4-O-卤代酰基-4′-去甲基表鬼臼毒素类似物的合成与抗肿瘤活性J. 药学学报, 1993, 28(10): 758-761.
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SF Yin, ZG Wang, WY Ma, XH Chen, TD Wang , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-O-(HALOGENATED) ACYL-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(10): 758-761.
Citation: SF Yin, ZG Wang, WY Ma, XH Chen, TD Wang , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-O-(HALOGENATED) ACYL-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(10): 758-761.
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4-O-卤代酰基-4′-去甲基表鬼臼毒素类似物的合成与抗肿瘤活性

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-O-(HALOGENATED) ACYL-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES

    摘要
  • 摘要: 为考察4′-去甲表鬼臼毒素C4位上联结含卤素原子的酯化侧链时对化合物抗肿瘤活性的影响,设计并采用选择性酯化方法合成了9个新的4′-去甲基表鬼臼毒素酯化产物。其中标题化合物在L1210白血病肿瘤细胞与KB细胞的体外生长抑制试验中普遍表现出显著的抑制活性,大部分化合物活性超过依托泊甙。而普通脂酸酯的活性较弱。

     

    Abstract: A series of 4-(halogenated) acyl-4'-demethylepipodophyllotoxin analogues were conveniently synthesized by selective esterification in the presence of BF3·Et2O, and screened in vitro against L1210 leukemia and KB cells. Most of these compounds showed marked antitumor activity and exhibited more potent activity than that of etoposide.

     

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