Huang Yanmin, Wen Haiyan, Zheng Jiahua, Gan Chunfang, Pang Liping, Pang Chunling, Liu Xiaolan, Zhan Junyan, Cui Jianguo
a College of Chemistry and Material Science , Guangxi Teachers Education University , Nanning , China.
Nat Prod Res. 2019 Apr;33(8):1101-1105. doi: 10.1080/14786419.2018.1457662. Epub 2018 Mar 30.
Using cholesterol, stigmasterol and sitosterol as starting materials, a series of 7-subsitituted-ster-3-yl 2-methoxybenzoate analogs were prepared through reacting with 2-methoxybenzoyl chloride and introducing some function groups, such as carbonyl, hydroxyl and various thiosemicarbazones, at 7-position of steroidal nucleus. The structures of these new compounds were characterized by IR, NMR and HRMS. Their antiproliferative activities were evaluated by using several types of cancer cells. Interestingly, the compounds displayed potent antiproliferative activity against CNE-2 (nasopharyngeal carcinoma cell lines), BEL-7402 (human liver cancer cell lines) and HepG2 (human liver cancer cell lines), suggesting that they have potential to be drug candidates for cancer treatment.
以胆固醇、豆甾醇和谷甾醇为起始原料，通过与2-甲氧基苯甲酰氯反应，并在甾体核的7位引入一些官能团，如羰基、羟基和各种硫代半卡巴腙，制备了一系列7-取代-甾体-3-基2-甲氧基苯甲酸酯类似物。这些新化合物的结构通过红外光谱、核磁共振和高分辨质谱进行了表征。通过使用几种类型的癌细胞评估了它们的抗增殖活性。有趣的是，这些化合物对CNE-2（鼻咽癌细胞系）、BEL-7402（人肝癌细胞系）和HepG2（人肝癌细胞系）显示出强大的抗增殖活性，表明它们有潜力成为癌症治疗的候选药物。
