4-(2-酰胺基-2-乙氧羰基)乙硫基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成与抗肿瘤活性  

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-(2-AMIDO-2-ETHOXYCARBONYL)ETHYLSULEENYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES

作　　者：尹述凡[1] 马维勇[1] 王天都[1] 陈秀华[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9期668-672,共5页Acta Pharmaceutica Sinica

摘　　要：为考察4′-去甲基表鬼臼毒素4位上取代基结构变化与抗肿瘤活性的关系,设计并合成了23个标题化合物。体外L_(1210)白血病细胞与KB细胞生长抑制试验的结果表明,化合物11,16和18的抗肿瘤活性超过依托泊甙,化合物8的活性与依托泊甙相当。Twenty three 4-(2-amido-2-ethoxycarbonyl) ethylsulfenyl-4-deoxy-4'-demethylepipodophyllotoxin analogues were synthesized by three steps, in which trifluoroacetic acid was used as a condensation agent of 4'-demethylepipodophyllotoxin with L-cysteine ethyl ester hydrochloride without any protection of phenolic hydroxy and amino groups. All compounds were screened in vitro against L_(1210) leukemia and KB cells, in which, compounds 11, 16 and 18 exhibited more potent antitumor activity than 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]