胱胺衍生物的合成及抗非小细胞肺癌活性研究  

Synthesis and anti-NSCLC activity of cystamine derivatives

作　　者：许萍 丁锐 江娟 邹远军 郭牡丹 刘晶晶 郑一敏[1] XU Ping;DING Rui;JIANG Juan;ZOU Yuanjun;GUO Mudan;LIU Jingjing;ZHENG Yimin(College of Pharmacy and Bioengineering,Chongqing University of Technology,Chongqing 400050,China;Chengdu Yukang Science and Technology Co.Ltd,Chengdu 610000,Sichuan,China)

机构地区：[1]重庆理工大学药学与生物工程学院,重庆400050 [2]成都与康科技有限公司,四川成都610000

出　　处：《化学研究》2022年第1期37-41,共5页Chemical Research

基　　金：重庆市科委重点项目涪陵区中药产业科技支撑示范工程协同管理创新与应用研究(CSTC2014zkjccxyyBX0034)。

摘　　要：为寻求活性强的非小细胞肺癌(NSCLC)药物,设计合成了一系列胱胺衍生物4a~4g,并对其抗NSCLC活性进行了初步探讨。以胱胺为起始原料,经过加成、还原反应得到了目标化合物,采用CCK-8法对其抗NSCLC细胞增殖活性进行了测试。目标化合物4a~4g结构经ESI-MS、^(1)H-NMR、^(13)C-NMR谱确证。活性结果表明,目标化合物对NCI-H520细胞增殖具有不同程度的抑制活性(IC_(50)值为44.1、38.1、49.3、40.1、38.8、12.6、5.9μmol/L),其中化合物4f和4g的抑制活性优于对照药物吉非替尼(IC_(50)值为29.7μmol/L)。化合物4f和4g(IC_(50)值为12.6、5.9μmol/L)抗NCI-H520细胞增殖活性较强,值得深入研究。In order to search for NSCLC drugs with higher potency,a series of cystamine derivatives(4a~4g)were designed and synthesized,and their anti-NSCLC activities were preliminarily investigated.The target compounds were obtained from cystamine via addition and reduction reactions,then the anti-NSCLC activity of these compounds was tested by CCK-8 assay.The structures of the target compounds were confirmed by ESI-MS,^(1)H-NMR,and ^(13)C-NMR.Compounds 4a~4g displayed potent inhibitory activities on the proliferation of NSCLC cell line H520(IC_(50)=44.1,38.1,49.3,40.1,38.8,12.6,5.9μmol/L),Compounds 4f and 4g showed higher anti-proliferative activity on NCI-H520 cells than gefitinib(IC_(50)=29.7μmol/L).Compounds 4f and 4g(IC_(50)=12.6、5.9μmol/L)had high anti proliferation activity against NCI-H520 cells,which was worthy of further investigation.

关 键 词：非小细胞肺癌 胱胺衍生物 增殖活性 合成 

分 类 号：O625.6[理学—有机化学]