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

被引：2

作者：

Liu, Chi ^{[1
]}

Liu, Xinyue ^{[1
]}

Ma, Qing ^{[1
]}

Su, Fengyan ^{[1
]}

Cai, Enbo ^{[1
]}

机构：

[1] Jilin Agr Univ, Coll Chinese Med Mat, 2888 Xincheng St, Changchun 130118, Jilin, Peoples R China

来源：

MOLECULES | 2024年 / 29卷 / 11期

关键词：

isoliquiritigenin derivatives; cervical cancer; antitumor; PI3K/Akt/mTOR signaling pathway; CANCER; CHALLENGES; APOPTOSIS;

D O I：

10.3390/molecules29112641

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M) had a better inhibitory effect on human cervical cancer (Hela) than ISL (IC50 = 126.5 mu M), and it was superior to the positive drug 5-FU (IC50 = 33.59 mu M). The mechanism of the action experiment showed that compound 9 could induce Hela cell apoptosis and autophagy through the PI3K/Akt/mTOR pathway.

引用

页数：18

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