Synthesis and Antitumor Activity Study of Novel Formononetin Derivatives

Objective: In order to enrich the library of anti-tumor small molecule compounds, 8 compounds, with highly effective antitumor, have been designed and synthesized. Methods: MTT assay was used to detect the antiproliferation activity of 8 compounds on four human tumor cell lines (HCT-116, HeLa, DU-145, and SGC-7901). Cell cycle experiment, cell migration experiment, cell clone experiment and cell apoptosis experiment were used to study the antitumor mechanism of compound (V). Results: The compound (V) showed the strongest antitumor activity against the above four human tumor cells, especially against HCT-116 cells, with an IC₅₀ value of 4.21 ± 0.39 μM, which was significantly lower than that of cyclophosphamide. The results of a variety of cell experiments showed that the compound (V) significant antitumor activity, such as inhibiting the proliferation and migration of HCT-116 cells, arresting HCT-116 cells at S phase, and inducing apoptosis in HCT-116 cells. Discussion: Slight changes in the R group can cause significant changes in the in vitro antitumor activity, and when R is a strong electron donor group of ethyl L-tyrosinate, compound (V) exhibits the strongest inhibitory effect, with an IC₅₀ value of 4.21 ± 0.39 μM on HCT-116 cells. Conclusions: 8 compounds showed significant anti-tumor activity, and the compound (V), with a strong electron donor group of ethyl L-tyrosinate, showed the most significant effect, and the antiproliferation and antimigration effects of compound (V) was further investigated.