白藜芦醇衍生物的合成及抗乳腺癌活性研究  

Synthesis and Anti-breast Cancer Activity of Resveratrol Derivatives

作　　者：刘婉茹 张汭 李志 王月茹[1] 张翠亚 LIU Wan-ru;ZHANG Rui;LI Zhi;WANG Yue-ru;ZHANG Cui-ya(Xianyang Key Laboratory of Molecular Imaging and Drug Synthesis,School of Pharmacy,Shaanxi Institute of International Trade&Commerce,Xianyang 712046,China)

机构地区：[1]咸阳市分子影像与药物合成重点实验室,陕西国际商贸学院医药学院,陕西咸阳712046

出　　处：《精细化工中间体》2025年第2期31-34,共4页Fine Chemical Intermediates

基　　金：2024年陕西省大学生创新创业训练计划项目(S2024131230043);咸阳市分子影像与药物合成重点实验室项目(2021QXNL-PT-0008)。

摘　　要：报道了一类结构新颖的白藜芦醇衍生物的合成、表征及体外抗乳腺癌活性研究。在缩合剂N,N,N′,N′-四甲基-O-(7-氮杂苯并三唑-1-基)六氟磷酸脲(HATU)的作用下,白藜芦醇衍生物2分别与4种不同链长的二羧酸单酯3a~3d发生缩合反应,得到4种白藜芦醇衍生物1a~1d,产物结构经^(1)H NMR、ESI-MS表征。测试了4种产物对荷尔蒙依赖型乳腺癌细胞MCF-7和三阴性乳腺癌细胞MDA-MB-231的抗增殖活性。结果表明,白藜芦醇衍生物1a~1d对乳腺癌细胞MCF-7和MDA-MB-231均表现出明显抗增殖活性,对人正常乳腺上皮细胞MCF-10A没有明显毒性。The synthesis,characterization andin vitro anti-breast cancer activity of novel resveratrol derivatives were reported.Under the action of condensation agent N,N,N′,N′-tetramethyl-O-(7-azabenzo-1-yl)hexafluorophosphate urea(HATU),four resveratrol derivatives 1a~1d were synthesized by condensation reaction of resveratrol derivative 2 with four carboxylate esters 3a~3d with different chain lengths.The structures of the products were characterized by ^(1)H NMR and ESI-MS.Subsequently,the anti-proliferative activities of the four products against hormone-dependent breast cancer MCF-7 cells and triple-negative breast cancer MDA-MB-231 cells were tested.The results showed that the synthesized resveratrol derivatives 1a~1d exhibited obvious anti-proliferative activities against MCF-7 and MDA-MB-231 cells.In addition,the target compound showed no obvious toxicity to MCF-10A cells.

关 键 词：白藜芦醇衍生物 结构修饰 抗乳腺癌活性 

分 类 号：TQ463[化学工程—制药化工] O625.6[理学—有机化学]