College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
Steroids. 2014 Jan;79:14-8. doi: 10.1016/j.steroids.2013.10.011. Epub 2013 Nov 4.
Using cholesterol, stigmasterol and sitosterol as starting materials, some 4,6-diaza-A,B-dihomo-steroid bilactams were synthesized via two different synthetic routes by oxidation, reduction, oximation, Beckman rearrangement, etc. The cytotoxic activity of the synthesized compounds against SGC 7901 (human ventriculi carcinoma), Bel-7404 (human liver carcinoma), HeLa (human cervical carcinoma) and HT-29 (colonic carcinoma) cancer cells were investigated. The results showed that compounds 2 and 7b displayed a good cytotoxic activity to the SGC 7901, Bel 7404 and HeLa tumor cell lines with the IC50 values of 11.6, 16.4, 13.9 and 13.1, 21.8, 13.1 μmol/L, respectively. Their cytotoxic activity is almost same as cisplatin to these cells. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.
以胆固醇、豆甾醇和谷甾醇为起始原料，通过氧化、还原、肟化、贝克曼重排等反应，采用两种不同的合成路线合成了一些 4,6-二氮杂-A,B-二氢同型甾体双内酰胺。研究了合成化合物对 SGC 7901（人胃癌）、Bel-7404（人肝癌）、HeLa（人宫颈癌）和 HT-29（结肠癌）癌细胞的细胞毒性活性。结果表明，化合物 2 和 7b 对 SGC 7901、Bel 7404 和 HeLa 肿瘤细胞系具有良好的细胞毒性活性，IC50 值分别为 11.6、16.4、13.9 和 13.1、21.8、13.1μmol/L，与顺铂对这些细胞的活性相当。这些研究获得的信息可能有助于设计新型化疗药物。
