摘要
研究鬼臼毒素衍生物的合成方法,获得高活性的抗肿瘤新化合物。本文以鬼臼毒素为起始原料,在CF3COOH/NaI或者ZrCl4/NaBr的作用下,经SN1亲核取代,缩合,得到目标产物。该化合物通过1H NMR、MS谱确证,同时采用MTT法评价了新化合物的体外抗肿瘤活性。结果显示:目标化合物的体外抗肿瘤活性与依托泊苷相当,值得进一步研究。
The aim of this study was to develop a new synthetic method for the synthesis of podophyllotoxin derivative and to investigate the antitumor activity of the synthesized compound. The podophyllotoxin derivative was synthesized using podophyUotoxin as the starting material through a two-step processes including SN1 nucleophilic displacemem followed by condensationhydrolysis. The targeted compound was identified by 1^H NMR, MS. The arititumor activity of the compound was investigated by MTT assay. The results showed that the cytotoxicity of the new compound was similar to that of etopo-side.
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2014年第4期594-596,共3页
Natural Product Research and Development
基金
开封市科技计划项目(110374)
关键词
鬼臼毒素
表鬼臼毒素
合成
抗肿瘤活性
podophyllotoxin
epipodophyllotoxin
synthesis
antitumor activity
