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汉防己甲素衍生物的合成及其生物活性

郭威凤 许晋芳 刘锐玲 赵正保 郭跃伟

应用化学2017,Vol.34Issue(7):789-794,6.
应用化学2017,Vol.34Issue(7):789-794,6.DOI:10.11944/j.issn.1000-0518.2017.07.160514

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

郭威凤 1许晋芳 1刘锐玲 1赵正保 1郭跃伟2

作者信息

  • 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
  • 折叠

摘要

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.

关键词

汉防己甲素/Suzuki反应/CCK-8法/抗肿瘤活性

Key words

tetrandrine/Suzuki coupling reaction/cell counting kit-8 method/anti-tumor activity

分类

化学化工

引用本文复制引用

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):789-794,6.

应用化学

OA北大核心CSCDCSTPCD

1000-0518

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