Design, Synthesis, and Antitumor Activity of Isoliquiritigenin Amino Acid Ester Derivatives.
Chi LiuXinyue LiuQing MaFengyan SuEn-Bo CaiPublished in: Molecules (Basel, Switzerland) (2024)
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 1 H NMR and 13 C NMR. Among them, compound 9 (IC 50 = 14.36 μM) had a better inhibitory effect on human cervical cancer (Hela) than ISL (IC 50 = 126.5 μM), and it was superior to the positive drug 5-FU (IC 50 = 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.
Keyphrases
- amino acid
- magnetic resonance
- high resolution
- endothelial cells
- solid state
- papillary thyroid
- oxidative stress
- cell cycle arrest
- signaling pathway
- endoplasmic reticulum stress
- induced pluripotent stem cells
- emergency department
- squamous cell carcinoma
- mass spectrometry
- human health
- replacement therapy
- electronic health record