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

作　　者：尹述凡[1] 王志光[1] 马维勇[1] 陈秀华[1] 王天都[1] 张椿年[1] 

机构地区：[1]上海医药工业研究院,上海200437

出　　处：《药学学报》1993年第10期758-761,共4页Acta Pharmaceutica Sinica

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.

关 键 词：鬼臼毒素 衍生物 抗肿瘤活性 

分 类 号：R979.1[医药卫生—药品]