摘要
为考察4′-去甲表鬼臼毒素C_4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L_(1210)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。
A series of 4-(halogenated) acyl-4'-demethylepipodophyllotoxin analogues were conveniently synthesized by selective esterification in the presence of BF_3·Et_2O, and screened in vitro against L_(1210) leukemia and KB cells. Most of these compounds showed marked antitumor activity and exhibited more potent activity than that of etoposide.
出处
《药学学报》
CAS
CSCD
北大核心
1993年第10期758-761,共4页
Acta Pharmaceutica Sinica
关键词
鬼臼毒素
衍生物
抗肿瘤活性
4-(Halogenated)acyl-4′-demethylepipodophyllotoxin analogues
Antitumor activity
