Gan Chunfang, Cui Jianguo, Su Shaoyang, Lin Qifu, Jia Linyi, Fan Lianghua, Huang Yanmin
College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
Steroids. 2014 Sep;87:99-107. doi: 10.1016/j.steroids.2014.05.026. Epub 2014 Jun 11.
Steroidal thiosemicarbazones, semicarbazones and hydrazones have received extensive attention of scientists recently because they exhibit some biological activities such as antibacterial, antiviral and anticancer. Using different steroids as starting materials, through different chemical methods, 24 steroidal compounds with thiosemicarbazone, semicarbazone or hydrazone groups in their structures, were synthesized, characterized by IR, NMR and MS. The antiproliferative activity of the compounds was evaluated against human gastric cancer (SGC-7901) and human liver cancer (Bel-7404) cells. The structure-activity relationship of these compounds was discussed. The results showed that compound 3 and 12a-12c exhibited significant inhibitory activity to Bel-7404 cells, and IC50 values of them were 4.2, 11.0, 7.4 and 15.0μM respectively (Cisplatin, IC50: 11.6μM).
甾体类缩氨基硫脲、缩氨基脲和腙最近受到了科学家们的广泛关注，因为它们具有一些生物活性，如抗菌、抗病毒和抗癌活性。以不同的甾体为起始原料，通过不同的化学方法，合成了24种结构中含有缩氨基硫脲、缩氨基脲或腙基团的甾体化合物，并通过红外光谱（IR）、核磁共振（NMR）和质谱（MS）对其进行了表征。评估了这些化合物对人胃癌（SGC - 7901）和人肝癌（Bel - 7404）细胞的抗增殖活性。讨论了这些化合物的构效关系。结果表明，化合物3和12a - 12c对Bel - 7404细胞表现出显著的抑制活性，它们的半数抑制浓度（IC50）值分别为4.2、11.0、7.4和15.0μM（顺铂，IC50：11.6μM）。
