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
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.