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

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.

A series of hybrid imidazole compounds have been prepared from cholesterol, stigmasterol and di- osgenin.Their structures were confirmed by I H NMR, 13C NMR, HRMS and IR.These compounds have been eval- uated 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）.