甾体-咪唑盐杂合物的设计、合成及细胞毒活性研究

Design,synthesis and cytotoxic activity of novel hybrid compounds between steroid and imidazolium salts

摘要: 从胆甾醇、豆甾醇、薯蓣皂素出发合成了一系列新型的甾体咪唑盐化合物,其结构经1H NMR、13C NMR、HRMS以及IR波谱确定.对合成的新化合物进行了体外抗肿瘤细胞活性筛选,结果表明,发现3-苄基-1-(2α-胆甾-4-烯-3-酮)咪唑-3-溴盐(10)和3-胡椒苄基-1-(2α-胆甾-4-烯-3-酮)咪唑-3-溴盐(13)具有较好的体外肿瘤生长抑制活性,对乳腺癌细胞株Bcap-37的活性明显优于顺铂.

Abstract: A series of hybrid imidazole compounds have been prepared from cholesterol,stigmasterol and diosgenin.Their structures were confirmed by 1H NMR,13C NMR,HRMS and IR.These compounds have been evaluated in vitro against a panel of human tumor cell lines.The results showed that 3-benzly-1-(2α-cholest-4-en-3-one)imidazol-3-ium bromide (10) and 3-(3’,4’-methylenedioxy- benzyl) -1-(2α-cholest-4-en-3-one)imidazol-3-ium bromide (13) exhibited higher inhibitory activities against human breast cancer Bcap-37 than cisplatin (DDP).