化学学报 ›› 1993, Vol. 51 ›› Issue (9): 933-936. 上一篇    

研究论文

4-烷硒基-4-脱氧-4'-去甲表鬼臼毒素衍生物的合成和抗肿瘤活性

王志光;马维勇;张椿年   

  1. 国家医药管理局上海医药工业研究院
  • 发布日期:1993-09-15

Synthesis and antitumor activities of 4-alkylselenyl-4-deoxy-4'- demethylepipodophyliotoxin

WANG ZHIGUANG;MA WEIYONG;ZHANG CHUNNIAN   

  • Published:1993-09-15

4-溴-4-脱氧-4'-去甲表鬼臼毒素与硒脲作用生成假硒脲盐.该化合物在三乙胺作用下转化为类似于硒醇的不稳定中间体;而在氮气保护下,与活泼卤代烃室温反应即可得到相应的硒醚.六个硒取代的化合物均显示良好的体外抑制L1210及KB细胞活性.

关键词: 三乙胺 P, 硒化合物, 鬼桕毒, 抗肿瘤药, 去甲表鬼臼毒素, 去甲表鬼臼毒素, 硒脲

Reaction of 4-bromo-4-deoxy-4'-demethylepipodophyllotoxin with selenourea followed by displacement with active alkyl halides in the presence of Et3N gave 4-alkylselenyl-4-deoxy-4'-demethylepipodophyllotoxins. Six compounds containing Se, e.g. I, showed marked antitumor activities.

Key words: TRIETHYL AMINE P, SELENIUM COMPOUNDS, PODOPHYLLOTOXIN, ANTITUMOR DRUGS, SELENOUREA

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