论文部分内容阅读
从去氢表雄酮出发,通过官能团保护、臭氧化开环、环化反应,然后通过不同的化学反应及官能团转换,在甾核的不同位置引入不同官能团,合成了系列具有[6-5-6-5]-甾核结构的化合物。采用Hela(宫颈癌细胞株),Bel 7404(肝癌细胞株)和SGC 7901(胃癌细胞株)肿瘤细胞株,对这些化合物进行了体外抗肿瘤活性测试。研究结果表明,当C-6为缩氨硫腙基、C-17为肟基取代时,所得到的B-降-3-乙酰氧基-5-羟基-17-肟-雄甾-6-缩胺硫腙对HeLa细胞具有中等强度的细胞毒性。
Starting from dehydroepiandrosterone, different functional groups were introduced at different positions of steroidal nucleus through functional groups protection, ozonization ring-opening and cyclization reaction, and then through different chemical reactions and functional group conversion, a series of [6-5- 6-5] - steroidal structure. In vitro antitumor activity of these compounds was tested using Hela (cervical cancer cell line), Bel 7404 (liver cancer cell line), and SGC 7901 (gastric cancer cell line) tumor cell lines. The results show that when C-6 is thiadiazone and C-17 is substituted with oxime, the obtained B-nor-3-acetoxy-5-hydroxy-17-oxime-androst- Thiazide has moderate cytotoxicity on HeLa cells.