4-S-(5-酰氨基-1,3,4-噻二唑-2-基)-4-脱氧-4′-去甲基表鬼臼毒素衍生物的合成与抗肿瘤活性  

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-S-(5-AMIDO-1,3,4-THIODIAZOL-2-YL)4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES

作　　者：尹述凡[1] 庄武[1] 马维勇[1] 王志光[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10期762-765,共4页Acta Pharmaceutica Sinica

摘　　要：基于在4′-去甲基表鬼臼毒素母核C_4位上联结含有杂原子的芳香环取代基,以此考察其结构与活性关系的设想,设计并合成了10个标题化合物。体外L_(1210)白血病细胞与KB细胞生长抑制试验结果表明,这类化合物有较强的抗肿瘤活性。其中化合物SIPI-92-1772,1774,1775,1776,1777与1779的活性超过临床用药依托泊甙。其余化合物活性与依托泊甙相当或略低。By the condensation of 4'-demethylepipodophyllotoxin with 2-amino-5-mereapto-1,3, 4-thiodiazole in CF_3COOH and acylation in the presence of DEPC, 10 title compounds wereconveniently synthesized. These compounds were screened in vitro against L_(1210) leukemia and KB cells,in which compounds SIPI-92-1772, 1774, 1775, 1776, 1777 and 1779 exhibited more potent antitumor activity.

关 键 词：鬼臼毒素 抗肿瘤活性 

分 类 号：R979.1[医药卫生—药品]