新型苯并异喹啉类衍生物的设计、合成及抗辐射活性  

Design,Synthesis and Anti-radiation Activities Evaluation of Novel Benzoisoquinoline Derivatives

作　　者：杨洋 黄林峰 梁妍 李铭东 吴诗 胡文祥 李庶心 陈梦雅 YANG Yang;HUANG Lin-feng;LIANG Yan;LI Ming-dong;WU Shi;HU Wen-xiang;LI Shu-xin;CHEN Meng-ya(School of Pharmacy,Department of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China;Institute of Radiation Medicine,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China;School of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330006,China;School of Pharmacy,Hubei University of Science and Technology,Xianning 437100,China;Jingdong Xianghu Microwave Chemistry,The Joint Laboratory of Beijing Excalibur Space Military Academy of Medical Sciences,Beijing 101601,China)

机构地区：[1]广东药科大学药学院,广东广州510006 [2]军事科学院军事医学研究院辐射医学研究所,北京100850 [3]江西中医药大学药学院,江西南昌330006 [4]湖北科技学院药学院,湖北咸宁437100 [5]北京神剑天军医学科学院京东祥鹄微波化学联合实验室,北京101601

出　　处：《合成化学》2020年第11期933-940,共8页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(81573344)。

摘　　要：分别以5-氯戊酸或4-(氯甲基)苯甲酸为原料,经取代、成酰胺和水解反应合成了14个新型苯并异喹啉类衍生物(I1~I7和II1~II7),其结构经1H NMR和HR-MS(ESI)表征。通过MTS法检测HUVEC细胞在辐射照射后的增殖活性,结果显示:化合物I1和I2具有抗辐射活性,其细胞存活率分别为64.68±1.04*#和58.95±1.34*#。Using 5-chloropentanoic acid or 4-(chloromethyl)benzoic acid as raw materials,14 new benzisoquinoline derivatives(I1~I7 and II1~II7)were synthesized through substitution,amide formation and hydrolysis reactions.The structures were characterized by 1H NMR and HR-MS(ESI).The anti-radiation activity of the compounds was evaluated by MTS assay.Preliminary pharmacological results had shown that compounds I1 and I2 have anti-radiation activity,and their cell survival rates were 64.68±1.04*#and 58.95±1.34*#,respectively.

关 键 词：2-((((4-(1 3-二氧代-1H-苯并[异]异喹啉-2(3H)-基)丁基)氨基)磺酰基)-苯甲酸 溶血磷脂酸2受体 抗辐射 合成 苯并异喹啉 

分 类 号：O621.3[理学—有机化学]