Synthesis of Tetrandrine Derivatives and Their Biological Activity

doi:10.11944/j.issn.1000-0518.2017.07.160514

Chinese Journal of Applied Chemistry ›› 2017, Vol. 34 ›› Issue (7): 789-794.DOI: 10.11944/j.issn.1000-0518.2017.07.160514

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Synthesis of Tetrandrine Derivatives and Their Biological Activity

GUO Weifeng^a,XU Jinfang^a,LIU Ruiling^a,ZHAO Zhengbao^a^*(),GUO Yuewei^b

^aSchool of Pharmaceutical Science,Shanxi Medical University,Taiyuan 030001,China
^bChinese Academy of Sciences,Shanghai Institute of Materia Medica,Shanghai 201203,China

Received:2016-12-21 Accepted:2017-03-29 Published:2017-07-04 Online:2017-07-04
Contact: ZHAO Zhengbao

Abstract

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

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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Synthesis of Tetrandrine Derivatives and Their Biological Activity

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