中文关键词:孕烯醇酮水杨酸甲醚合成抗肿瘤活性 英文关键词:pregnenlonesalicylic acid methyl ethersynthesisantiproliferative activity 基金项目:国家自然科学基金项目

作者	单位	E-mail
刘志平	南宁师范大学化学与材料学院	liuzhiping828@126.com
祝志凌	南宁师范大学化学与材料学院
郑嘉桦	南宁师范大学化学与材料学院
甘春芳	南宁师范大学化学与材料学院
黄燕敏	南宁师范大学化学与材料学院
崔建国	南宁师范大学化学与材料学院

摘要点击次数:1091 全文下载次数:0 中文摘要: 从孕烯醇酮出发,通过酯化反应在3-位羟基上引入不同结构酯链,再对20-位羰基进行结构修饰,合成了10个(20R)-孕甾-5-烯-20-(2-甲氧基苯甲酸酯)类化合物,并通过IR、NMR及HRMS方法进行了结构表征。合成的化合物用噻吩蓝比色法(MTT)体外测试了对人宫颈癌细胞(HeLa)、人肺癌细胞(A549)、人甲状腺癌细胞(TPC-1)、人鼻炎癌细胞(CNE-2)以及人正常肾上皮细胞(HEK-293T)的增殖生长抑制活性,结果显示化合物2d和3d对A549的抑制效果显著,其IC₅₀达到了7.9 μM和10.3 μM,而对人正常肾上皮细胞 HEK-293T细胞无毒性。 英文摘要: Using pregnenlone as a raw material, ten (20R)-pregn-5-ene-20-(2-methoxybenzoate) compounds were designed and synthesized by esterification on 3-hydroxyl group and structural modification on 20-carbonyl group. Their structures were determined by IR, NMR and HRMS. The antiproliferative activity of the target compounds were evaluated against HeLa (human cervical cancer), A549 (Human lung cancer), TPC-1(Human thyroid cancer), CNE-2 (nasopharyngeal carcinoma) and human HEK-293T (Normal Kidney Epithelial) by MTT method in vitro. The results showed that the compounds 2d and 3d displayed distinct antiproliferative activity against A549 with the values of IC₅₀ 7.9 and 10.3 μM, and were almost inactive to HEK-293T cells. 查看全文查看/发表评论下载PDF阅读器 相关附件：版权转让声明书附件1论文修改稿附件1 -->