Cui Jianguo, Pang Liping, Wei Meizhen, Gan Chunfang, Liu Dandan, Yuan Haiyan, Huang Yanmin
College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, PR China; College of Petroleum and Chemical Engineering, Qizhou University, Qizhou, PR China.
College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, PR China.
Steroids. 2018 Dec;140:151-158. doi: 10.1016/j.steroids.2018.10.004. Epub 2018 Oct 6.
Using pregnenolone as a starting material, some 3-substituted 17-[1',2',3']-selenadiazolylpregnenolone derivatives were synthesized, and their structures were characterized by IR, NMR and HRMS. The in vitro antitumor activity of the compounds was assayed against PC-3、SKOV3、T47D、MCF-7 and HEK293T cell lines. The results show that some compounds display selective antiproliferative activity against PC-3 and SKOV3 cells lines and are almost inactive to normal kidney epithelial cells (HEK293T). The IC value are much better than that of abiraterone (positive control).
以孕烯醇酮为起始原料，合成了一些3-取代的17-[1',2',3']-硒二唑基孕烯醇酮衍生物，并通过红外光谱、核磁共振和高分辨质谱对其结构进行了表征。测定了这些化合物对PC-3、SKOV3、T47D、MCF-7和HEK293T细胞系的体外抗肿瘤活性。结果表明，一些化合物对PC-3和SKOV3细胞系具有选择性抗增殖活性，而对正常肾上皮细胞（HEK293T）几乎无活性。其半数抑制浓度值比阿比特龙（阳性对照）要好得多。
