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Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents

文献类型： 外文期刊

作者： Li, Dechao 1 ; Liu, Haizheng 1 ; Liu, Yufa 1 ; Zhang, Qikun 1 ; Liu, Chao 2 ; Zhao, Shuhua 3 ; Jiao, Bo;

作者机构： 1.Shandong Normal Univ, Collaborat Innovat Ctr Functionalized Probes Chem, Coll Chem Chem Engn & Mat Sci,Key Lab Mol & Nano, Minist Educ,Shandong Prov Key Lab Clean Prod Fine, 88 East Wenhua Rd, Jinan 250014, Peoples R China

2.Shandong Acad Agr Sci, Inst Agrofood Sci & Technol, 202 Gongye North Rd, Jinan 250100, Peoples R China

3.Shandong Acad Agr Sci, I

关键词： Tetrandrine;Fangchinoline;Anti-tumor activity;Apoptosis

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS （ 影响因子：2.823； 五年影响因子：2.677 ）

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： The isolation and modification of natural products is always a very important resources to anti-tumor drugs. Therefore, a novel series of tetrandrine and fangchinoline derivatives were designed and synthesized, and their antiproliferative activities against HepG2, MCF-7 cells were evaluated and described. From the activity result obtained, high to very high activity in vitro has been found, one of the tested compounds (compound 5d) exhibited the most significant cytotoxic effects. Compound 5d increased 29.2, 7.37 times anti-proliferative activity for HepG2 cells and MCF-7 cells compared to sunitinib (IC50 = 16.06 mu M and 25.41 mu M). Finally flow cytometry determined that compound 5d could indeed inhibit the proliferation of HepG2 cells via inducing apoptosis. (C) 2016 Elsevier Ltd. All rights reserved.

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