新型异吲哚酮衍生物的合成与活性研究  

Synthesis and Biological Activities of Novel Isoindolinone Derivatives

作　　者：曹瑞霞 贾玉萍 CAO Rui-xia;JIA Yu-ping(College of Chemistry and Chemical Engineering, Qilu Normal University, Ji’nan 250200, China;Shandong Academy ofPharmaceutical Sciences, Ji’nan 250101, China)

机构地区：[1]齐鲁师范学院化学与化工学院,山东济南250200 [2]山东省药学科学院,山东济南250101

出　　处：《合成化学》2022年第2期90-97,共8页Chinese Journal of Synthetic Chemistry

基　　金：山东省高校科技计划项目(J16LC52);齐鲁师范学院青年博士支持计划资助项目(QBJH19-0038);济南市“高校20条”资助项目(引进创新团队2019GXRC039,2020GXRC043);齐鲁师范学院校级青年项目(2015L0604)。

摘　　要：为了寻找结构新颖,活性较好的抗肿瘤化合物,本文设计并合成了15个未见报道的异吲哚酮衍生物(Ⅰ_(1)~Ⅰ_(5),Ⅱ_(1)~Ⅱ_(5)和Ⅲ_(1)~Ⅲ_(5)),其结构经^(1)H NMR和HR-MS(ESI)表征。使用四甲基偶氮唑盐(MTT)法,初步的生物活性测试结果表明:部分化合物对人肺癌细胞A549(Ⅱ_(4),IC_(50)=15.49μM)、人结肠癌细胞Colo205(Ⅱ_(4),IC_(50)=15.54μM)、人胰腺癌细胞PNAC-1(Ⅱ_(4),IC_(50)=37.07μM)和人骨髓瘤细胞U266(Ⅱ_(5),IC_(50)=75.27μM)表现出明显的抑制作用。15 new isoindolinone derivatives(Ⅰ_(1)~Ⅰ_(5),Ⅱ_(1)~Ⅱ_(5) and Ⅲ_(1)~Ⅲ_(5)) were synthesized and characterized by 1H NMR and HR-MS(ESI).Preliminary in vitro tests for human lung cancer cell lines A549(Ⅱ_(4),IC_(50)=15.49μM),human colon cancer cell Colo205(Ⅱ_(4),IC_(50)=15.54μM),human pancreatic carcinoma cell PNAC-1(Ⅱ_(4),IC_(50)=37.07μM)and human myeloma cell U266(Ⅱ_(4),IC_(50)=75.27μM)activity of these isoindolone derivatives by the method of MTT,the results indicated that most of them exhibit good inhibitory activity.

关 键 词：异吲哚酮 抗肿瘤 合成 人肺癌细胞 人结肠癌细胞 人胰腺癌细胞 人骨髓瘤细胞 

分 类 号：O625[理学—有机化学]