4-(2-氨基-2-环戊氧羰基)乙硫基-4-脱氧-4′-去甲基表鬼臼毒素及其酰化衍生物的合成与抗肿瘤活性  

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-(2-AMINO-2-CYCLOPENTYLOXYCARBONYL)-ETHYLTHIO-4-DEOXY-4＇-DEMETHYLEPIPODOPHYLLOTOXIN AND ITS ACYL DERIVATIVES

作　　者：尹述凡[1] 马维勇[1] 王志光[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20043

出　　处：《中国医药工业杂志》1993年第6期250-253,共4页Chinese Journal of Pharmaceuticals

摘　　要：为了考察鬼臼毒素 C_4位侧链取代基变化对活性的影响,合成28个标题化合物。体外 L1210白血病细胞及 KB 细胞生长抑制试验结果,表明所有化合物均具不同程度的抗肿瘤活性,其中化合物(1)、(5)和(8)～(10)的活性超过临床用药依托泊甙。Twenty seven 4-(2-amido-2-cyclopentyloxycarbonyl) ethylthio 4-deoxy-4'-demethylepipodophyllotoxin derivative were synthesized and screened invitro against L1210 and KB cells.Among them,compounds (1),(5),and (8)～(10)exhibited more potent antitumor activity than etoposide.

关 键 词：表鬼臼毒素 合成 抗肿瘤活性 

分 类 号：R979.1[医药卫生—药品]