咪唑并[1,2-a]喹喔啉衍生物的合成及其体外抗乳腺癌活性研究  

Study on the Synthesis and Antitumor Activity of Imidazo[l,2-a]Quinoxalines

作　　者：林晨[1] 许贻文 柯方[1,2] 陈晓乐[1,2] 许建华[1,2] 林媚[1] LIN Chen;XU Yiwen;KE Fang;CHENXiaole;XU Jianhua;LIN Mei(Department of Pharmacology,Fujian Medical University,Fuzhou 350122,China;New Drug Research Institute,Fujian Medical University,Fuzhou 350122,China)

机构地区：[1]福建医科大学药学院,福州350122 [2]福建医科大学新药研究所,福州350122

出　　处：《福建医科大学学报》2018年第6期355-358,共4页Journal of Fujian Medical University

基　　金：国家自然科学基金(81402842);福建省科技厅研究基金(2016J01686;2016J01372;2016Y9051;2017J01820;2015J01316);福建医科大学苗圃基金(2015MP008)

摘　　要：目的合成咪唑并[1,2-a]喹喔啉衍生物,并检测其体外抗乳腺癌活性研究。方法以2-氯甲基苯并咪唑和N-4-甲苯磺酰基-2-氨基碘苯为底物,通过微波辐射催化法合成咪唑并[1,2-a]喹喔啉衍生物。细胞划痕实验和MTT法测定合成的化合物的体外抗肿瘤活性。结果化合物c和e的半数抑制浓度均低于其他吡咯并[1,2-a]喹喔啉化合物。结论化合物c和e均具有抗肿瘤活性,可作为针对SKBR3和MCF-7细胞开发出耐受性好、毒副作用小的新型抗肿瘤药物。Objective To synthesis imidazo[1,2-a]quinoxalines derivatives and test their antitumor activity.Methods Microwave-assisted organic synthesis of imidazo[1,2-a]quinoxalines derivatives through the reaction of N-(2-iodophenyl)-4-methyl-benzenesulfonamid with 2-(chloromethyl)-1H-benzo[d]imidazoles was investigated.Their in vitro antitumor activities were evaluated by wound healing and MTT.Results These data showed that compounds c and e were less active than other compounds.Conclusion These new compounds are able to inhibit proliferation of SKBR3 and MCF-7 breast cancer cells.Therefore,the structure of imidazo[1,2-a]quinoxalines can be optimized to promote the anticancer activity of quinoxaline derivatives.

关 键 词：乳腺肿瘤 抗肿瘤药 工艺学 制药 

分 类 号：R454.1[医药卫生—治疗学] R730.2[医药卫生—临床医学]