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Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives

Journal 2020 · IF 1.863 · 43(1): 102-109 · 发表于 2020 年 1 月 1 日
作者: Qing-Xuan Zheng,Rui Wang,Yan Xu,Chang-Xin He,Cai-Yun Zhao,Zhi-Fang Wang,Rui Zhang,Wim Dehaen,Hui-Jing Li,Qi-Yong Huai
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摘要

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 20 µM, respectively.