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.
出处
《药学学报》
CAS
CSCD
北大核心
1993年第10期762-765,共4页
Acta Pharmaceutica Sinica
关键词
鬼臼毒素
抗肿瘤活性
Podophyllotoxin
4-S-(5-Amido-1
3
4-thiodiazol-2-yl)4-deoxy-4'-demethylepi-podophyllotoxin analogues
Antitumor activity
