N-芳乙基异喹啉衍生物的合成及其抗肿瘤活性研究  

Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents

作　　者：汪燕翔[1] 赵午莉[1] 毕重文[1] 李阳彪[1] 邵荣光[1] 宋丹青[1] 

机构地区：[1]中国医学科学院、北京协和医学院医药生物技术研究所,北京100050

出　　处：《药学学报》2012年第2期200-205,共6页Acta Pharmaceutica Sinica

基　　金："十二五重大新药创制"科技重大专项资助项目(2012ZX09301002-001-017)

摘　　要：本研究采用一种简便的新方法设计合成了一系列全新结构的N-芳乙基异喹啉衍生物,并对其体外抗肿瘤活性进行了评价。其中化合物9a表现出较强的抗肿瘤活性,对人肝癌HepG2和大肠癌HCT116细胞的IC50值分别为2.52和1.99μg.mL–1。初步作用机制显示,9a可以将HepG2细胞周期阻滞于S期,使细胞增殖受阻,达到抗肿瘤效果。A series of novel N-（2-arylethyl） isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities. Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC50 values of 2.52 and 1.99μg·mL^-1, respectively. Cell cycle was blocked at S phase of HepG2 cells treated with 9a by flow cytometry detection. Our results provided a basis for the development of a new series of anti-cancer candidates.

关 键 词：N-芳乙基异喹啉 抗肿瘤 构效关系 

分 类 号：R916[医药卫生—药学]