二氢青蒿素-碱基拼合物的合成及抗肿瘤活性研究  

Synthesis and anti-tumor activity of dihydroartemisinin-base hybrids

作　　者：李冰清 丁洁 夏凯 宋雨阳 艾义 朱俊杰 钟杭 LI Bing-qing;DING Jie;XIA Kai;SONG Yu-yang;AI Yi;ZHU Jun-jie;ZHONG Hang(School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《化学研究与应用》2022年第6期1385-1393,共9页Chemical Research and Application

基　　金：贵州省科技计划项目([2019]1121)资助;贵州大学培育项目([2020]83)资助。

摘　　要：以二氢青蒿素为先导化合物,设计并合成15个二氢青蒿素-碱基拼合物(LA01~LA13,LB01,LB02),化合物结构经^(1)HNMR和ESI-MS表征。采用MTT法测定LA和LB系列化合物对乳腺癌MDA-MB-436和T47D细胞株的体外抗增殖活性。结果表明,化合物LA13和LB01对三阴乳腺癌MDA-MB-436细胞有显著抑制活性,其IC_(50)值分别为5.32μmol·L^(-1)和2.54μmol·L^(-1)。Fifteen dihydroartemisinin-base hybrids(LA01~LA13,LB01,LB02)were designed and synthesized based on the lead of dihydroartemisinin.These novel compounds were characterized by ^(1)HNMR and ESI-MS.The MTT method was employed to determine the in vitro anti-proliferative activity of LA and LB series compounds on breast cancer cell lines MDA-MB-436 and T47D.The results showed that compounds LA13 and LB01 had significant inhibitory activity on triple-negative breast MDA-MB-436 cells,with IC_(50)values of 5.32μmol·L^(-1)and 2.54μmol·L^(-1),respectively.

关 键 词：二氢青蒿素-碱基拼合物 合成 抗肿瘤 

分 类 号：O622.6[理学—有机化学]