Synthesis and Biological Evaluation of the Matrine Derivatives as a Novel Family of Potential Anticancer Agents

Author(s): Jing Wang, Hang Liu, Xiao-Bin Zhuo, Guang-Ming Ye, Qing-Jie Zhao*

Journal Name: Medicinal Chemistry

Volume 17 , Issue 5 , 2021

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Graphical Abstract:


Background: FufangKushen injection’ was a Chinese Traditional anticancer drug, which has been widely used to treat cancer in combination with other anticancer drugs.

Objective: Our goal is to synthesize a series of novel 13-dithiocarbamates matrine derivatives using matrine (1) as the lead compound, and evaluate the biological activities of the obtained compounds.

Methods: The in vitro cytotoxicity of the target compounds against three human cancer cell lines (Hep3B, LM3 and BeL-7404) was evaluated. To investigate the mechanism of biological activity, cell cycle analysis was performed.

Results: The results revealed that compounds 6o and 6v displayed the most significant anticancer activity against three cancer cell lines with IC50 values in the range of 3.42-8.05 μM, which showed better activity than the parent compound (Matrine). SAR analysis indicated that the introduction of a substituted amino dithiocarbamate might significantly enhance the antiproliferative activity.

Conclusion: During the newly synthesized compounds, matrine analog 6v exhibited a potent effect against three human tumor cell lines. The mode of action of 6v was to inhibit the G0/G1 phase arrest. Therefore, compound 6v has been selected as a novel-scaffold lead to further structural optimizations or as a chemical probe for exploring anticancer pathways of this kind of compounds.

Keywords: Matrine, alkaloids, derivatives, cell cycle, anti-cancer activity, SAR.

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Article Details

Year: 2021
Published on: 24 May, 2021
Page: [493 - 500]
Pages: 8
DOI: 10.2174/1573406415666191022145534
Price: $65

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