4,4’-O-双(2-羟基-3-取代氨基)丙基-4-去甲表鬼臼毒素的合成及抗肿瘤活性  

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4,4'-OBIS-(2-HYDROXY-3-SUBSTITUTED-AMINO) PROPYL-4'-DEMETHYLEPIPODOPHYLLOTOXINS

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：《中国医药工业杂志》1993年第11期486-488,513,共4页Chinese Journal of Pharmaceuticals

摘　　要：为探索鬼臼毒素C_4位侧链结构与活性的关系,合成了5个标题化合物。体外药理试验表明新化合物对L1210白血病细胞与KB细胞生长抑制作用普遍强于依托泊甙,提示含有羟基和氨基的侧链可能为出现活性所必需。Five 4,4'-O-bis(2-hydroxy-3-substituted-amino) propyl-4'-demethylepipodophyllotoxins were synthesized and screened with L 1210 leukemia and KB cells in vitro. All of them exhibited more potent antitumor activity than etoposide, which indicated that the side-chains containing hydroxy and amino groups may be one of the active zones in the structure of podophyllotoxins.

关 键 词：鬼臼毒素 合成 抗肿瘤活性 

分 类 号：TQ463[化学工程—制药化工]