Background: A natural compound (-)-β-pinene was used as a raw material, and twenty-six
novel derivatives with amide or acylthiourea groups were synthesized based on the molecular hybridization
Methods: In vitro antitumor activity of these derivatives on human breast cancer cell line MCF7 and
human colon cancer cell line SW1116 were tested. The effects of the synthesized derivatives on the
morphology of MCF7 and SW1116 were observed. The antitumor activity evaluation results show
that among these derivatives, compounds 5c, 5e, 5h, 7c, 7b and 7e exhibit good antitumor activity
against MCF7, and compounds 5c, 5e, 5h and 7j exert moderate antitumor activity against SW1116.
Results: The preliminary structure-activity relationship analysis demonstrates that the position and
species of substituents on the aromatic ring of derivatives have an effect on the antitumor activity of
derivatives. Observation of the cell morphology reveals that derivatives with antitumor activity can
lead to rounding of the cell morphology, a decrease in cell volume and cell density, and ultimately
inhibition of the proliferation of MCF7 and SW1116 cells.
Conclusion: This study hopes to promote the high value-added utilization of natural compounds β-
pinene and the development of novel antitumor drugs.