汉防己甲素衍生物的合成及其生物活性  

Synthesis of Tetrandrine Derivatives and Their Biological Activity

作　　者：郭威凤 许晋芳[1] 刘锐玲[1] 赵正保[1] 郭跃伟[2] 

机构地区：[1]山西医科大学药学院,太原030001 [2]中国科学院上海药物研究所,上海201203

出　　处：《应用化学》2017年第7期789-794,共6页Chinese Journal of Applied Chemistry

摘　　要：为寻找更为有效的抗肿瘤药物,改善汉防己甲素的抗肿瘤活性,本文以汉防己甲素为原料,经过Suzuki反应设计并合成了6个新的双苄基异喹啉类衍生物。新化合物经过质谱(MS)、核磁共振氢谱(~1H NMR)、核磁共振碳谱(^(13)C NMR)等技术手段进行了结构确证。采用细胞计数试剂盒(CCK-8)法初步评价了6个新化合物对人肺癌细胞(A549)和小鼠白血病细胞(P388)的抗肿瘤活性。结果表明,化合物均有不同程度的抗肿瘤活性,其中化合物H1、H4、H6对A549细胞的抗肿瘤活性(IC50<10μmol/L)明显优于阳性对照汉防己甲素。In order to explore more effective anti-tumor drugs, and improve the anti-tumor activities of tetrandrine, six new bisbenzylisoquinoline derivatives of tetrandrine were designed and synthesized by Suzuki coupling. The structures of these compounds were confirmed by 1H nuclear magnetic resonance （ 1H NMR）, 13 C nuclear magnetic resonance （ 13 C NMR）, and mass spectrometry （MS）. Their inhibitory activities against human lung cancer cells （A549） and murine leukemia cells （P388） were evaluated by CCK-8 （cell counting kit-8） method. All these compounds exhibit a certain level of anti-tumor activities, while compounds HI, H4, H6 possess better cytotoxicity profile than tetrandrine against A549 cells.

关 键 词：汉防己甲素 SUZUKI反应 CCK-8法 抗肿瘤活性 

分 类 号：O629.3[理学—有机化学] O621.3[理学—化学]