汉防己甲素衍生物的合成及其生物活性

doi:10.11944/j.issn.1000-0518.2017.07.160514

摘要/Abstract

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(¹³C 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<10 μmol/L)明显优于阳性对照汉防己甲素。

关键词: 汉防己甲素, Suzuki反应, CCK-8法, 抗肿瘤活性

Abstract:

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),¹³C nuclear magnetic resonance(¹³C 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 H1, H4, H6 possess better cytotoxicity profile than tetrandrine against A549 cells.

Key words: tetrandrine, Suzuki coupling reaction, cell counting kit-8 method, anti-tumor activity

郭威凤, 许晋芳, 刘锐玲, 赵正保, 郭跃伟. 汉防己甲素衍生物的合成及其生物活性[J]. 应用化学, 2017, 34(7): 789-794.

GUO Weifeng, XU Jinfang, LIU Ruiling, ZHAO Zhengbao, GUO Yuewei. Synthesis of Tetrandrine Derivatives and Their Biological Activity[J]. Chinese Journal of Applied Chemistry, 2017, 34(7): 789-794.

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