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Synthesis and Biological Evaluation of matrine derivatives as a Novel Family of Potential Anticancer Agents

Author(s):

Jing Wang, Hang Liu, Xiao-Bin Zhuo, Guang-Ming Ye and Qing-Jie Zhao  

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 compounnd, and evaluate biological activities of obtained compounds.

Method: 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 were performed.

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

Conclusion: During the newly synthesized compounds, matrine analogue 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 for further structural optimizations or as a chemical probe for exploring anticancer pathways of this kinds of compounds.

Keywords:

Marine, Alkaloids, Derivatives, Cell cycle, Anti-cancer activity

Affiliation:

Huzhou Clinical College of Anhui medical University, No.98 Hospital of PLA, Huzhou 230032, Department of Organic Chemistry, Second Military Medical University, Shanghai 200433, Huzhou Clinical College of Anhui medical University, No.98 Hospital of PLA, Huzhou 230032, Huzhou Clinical College of Anhui medical University, No.98 Hospital of PLA, Huzhou 230032, Huzhou Clinical College of Anhui medical University, No.98 Hospital of PLA, Huzhou 230032



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