Design, Synthesis, and Antitumor Activity of Isoliquiritigenin Amino Acid Ester Derivatives

异甘草素氨基酸酯衍生物的设计、合成及抗肿瘤活性

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作者:Chi Liu, Xinyue Liu, Qing Ma, Fengyan Su, Enbo Cai

Abstract

Isoliquiritigenin (ISL) is a chalcone that has shown great potential in the treatment of cancer. However, its relatively weak activity and low water solubility limit its clinical application. In this study, we designed and synthesized 21 amino acid ester derivatives of ISL and characterized the compounds using 1H NMR and 13C NMR. Among them, compound 9 (IC50 = 14.36 μM) had a better inhibitory effect on human cervical cancer (Hela) than ISL (IC50 = 126.5 μM), and it was superior to the positive drug 5-FU (IC50 = 33.59 μM). The mechanism of the action experiment showed that compound 9 could induce Hela cell apoptosis and autophagy through the PI3K/Akt/mTOR pathway.

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