Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives

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Abstract

Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20µM, respectively.

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Zheng, Q. X., Wang, R., Xu, Y., He, C. X., Zhao, C. Y., Wang, Z. F., … Huai, Q. Y. (2020). Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives. Biological and Pharmaceutical Bulletin, 43(1), 102–109. https://doi.org/10.1248/bpb.b19-00615

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