桦木醇-28-吲哚腙衍生物的合成及生物活性研究  

Study on the Synthesis and Biological Activity of Betulin-28-indole Hydrazone Derivatives

作　　者：李登辉 华志鹏 楚蕾冰 李欢 李睿 卜明 Li Denghui;Hua Zhipeng;Chu Leibing;Li Huan;Li Rui;Bu Ming(School of Pharmacy,Qiqihar Medical University,Qiqihar 161006,China)

机构地区：[1]齐齐哈尔医学院药学院,黑龙江齐齐哈尔161006

出　　处：《广东化工》2023年第15期33-35,共3页Guangdong Chemical Industry

基　　金：黑龙江省大学生创新创业训练计划项目(X202211230045);齐齐哈尔医学科学院科研项目(QMSI2022Z-01)。

摘　　要：桦木醇抗肿瘤活性中等,极大限制了其进一步应用。为进一步提高其生物活性,本研究在桦木醇C-28位的羟基进行结构修饰,合成8个新型桦木醇-28-吲哚腙类衍生物,并采用1HNMR、13C NMR和HRMS进行结构表征。通过MTT法测试衍生物对人乳腺癌细胞(MCF-7)、人肝癌细胞(HepG2)和人结直肠癌细胞(HCT-116)的体外抗增殖活性。结果表明,化合物7c对三种肿瘤细胞株均表现出理想的抑制作用,对MCF-7细胞的抑制作用最强(IC_(50)=9.18μmol/L),具有深入研究价值。The moderate antitumor activity betulin greatly affects its further application.To further enhance its biological activity,eight new betulin-28-indole hydrazone derivatives were synthesized by structural modification of the hydroxyl group at C-28 of betulin and characterized by 1H NMR,13C NMR and HRMS.The in vitro antiproliferative activities of the derivatives against human breast cancer cells(MCF-7),human liver cancer cells(HepG2)and human colorectal cancer cells(HCT-116)were tested by MTT assay.The results showed that compound 7c showed desired inhibitory effect on all three tumor cell lines,and showed significant inhibitory effect on MCF-7 cells(IC_(50)=9.18μmol/L),which is valuable for further study.

关 键 词：桦木醇 结构修饰 吲哚 结构表征 抗肿瘤活性 

分 类 号：O626[理学—有机化学]