Abstract
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.
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The data that support the findings of this study are available from the corresponding author upon reasonable request.
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This work was financially supported by Guangxi Collaborative Innovation Center of Modern Sericulture and Silk (Grant no. 2022GXCSSC10) and High-level Talents Scientific Research Startup Fund of Hechi University (Grant no. 2019GCC008).
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Luo, Z., Pan, L., Yin, X. et al. Synthesis and Antitumor Activity Study of Novel Formononetin Derivatives. Russ J Bioorg Chem 50, 313–327 (2024). https://doi.org/10.1134/S1068162024020110
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DOI: https://doi.org/10.1134/S1068162024020110