4-β-取代氨基甲酰-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成及抗肿瘤活性  

Synthesis and Antitumor Activity of 4-β-Substituted Carbamoyl-4-deoxy-4′-demethylepipodophyllotoxin

作　　者：陈再新[1] 马维勇1 陈秀华[1] 王金娣[2] 张椿年[1] 

机构地区：[1]上海医药工业研究院,上海200040 [2]华东理工大学,上海200237

出　　处：《中国医药工业杂志》2000年第6期265-268,共4页Chinese Journal of Pharmaceuticals

摘　　要：为考察 4′-去甲表鬼臼毒素 C4 位上连接碳原子后对其生物活性的影响 ,本文设计并合成了 C4 位β构型取代氨基甲酰取代的衍生物 2 6个。它们在体外的抑制 L1 2 1 0细胞和 KB细胞的药理实验中 ,虽显示了一定的抗肿瘤细胞生长活性 。Twenty six 4 β substituted carbamoyl 4 deoxy 4′ demethylepipodophyllotoxins were synthesized, and screened in vitro against L1210 leukemia and KB cells. These compounds showed positive antitumor activities, but all were less potent than etoposide.

关 键 词：鬼臼毒素 衍生物 抗肿瘤活性 合成 

分 类 号：R979.11[医药卫生—药品] R914.5[医药卫生—药学]