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

Author:

Liu Chi1,Liu Xinyue1,Ma Qing1,Su Fengyan1,Cai Enbo1ORCID

Affiliation:

1. College of Chinese Medicinal Material, Jilin Agricultural University, 2888 Xincheng Street, Changchun 130118, China

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.

Funder

Jilin Province Science & Technology Development Plan

Publisher

MDPI AG

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