2. Academic Validation
  3. Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents

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

  • Bioorg Med Chem Lett. 2017 Feb 1;27(3):533-536. doi: 10.1016/j.bmcl.2016.12.029.
Dechao Li 1,  Haizheng Liu 1,  Yufa Liu 2,  Qikun Zhang 1,  Chao Liu 3,  Shuhua Zhao 3,  Bo Jiao 4
Affiliations

Affiliations

  • 1 College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Provincial Key Laboratory of Clean Production of Fine Chemicals, Shandong Normal University, 88 East Wenhua Road, Jinan 250014, PR China.
  • 2 College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Provincial Key Laboratory of Clean Production of Fine Chemicals, Shandong Normal University, 88 East Wenhua Road, Jinan 250014, PR China. Electronic address: liuyufa@sdnu.edu.cn.
  • 3 Institute of Agro-Food Science and Technology, Shandong Academy of Agricultural Sciences, 202 Gongye North Road, Jinan 250100, PR China.
  • 4 School of Medicine, Shandong University, 44 West Wenhua Road, Jinan 250012, PR China.
PMID: 28057423 DOI: 10.1016/j.bmcl.2016.12.029
Abstract

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=16.06μM and 25.41μM). Finally flow cytometry determined that compound 5d could indeed inhibit the proliferation of HepG2 cells via inducing Apoptosis.

Keywords

Anti-tumor activity; Apoptosis; Fangchinoline; Tetrandrine.

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