Synthesis and Biological Evaluation of Novel Furopyridone Derivatives As Potent Cytotoxic Agents Against Esophageal Cancer

Overview

Journal Int J Mol Sci

Publisher MDPI

Specialties Biochemistry
Chemistry
Molecular Biology

Date 2024 Sep 14

PMID 39273581

Authors

Xingyu Ren

Jiaojiao Zhang

Anying Dai

Pengzhi Sun

Yibo Zhang

Lu Jin

Le Pan

Affiliations

Soon will be listed here.

Abstract

Cancer continues to be a major global health issue, ranking among the top causes of death worldwide. To develop novel antitumor agents, this study focused on the synthesis of a series of 21 novel furanopyridinone derivatives through structural modifications and functional enhancements. The in vitro anti-tumor activities of these compounds were investigated through the cytotoxicity against KYSE70 and KYSE150 and led to the identification of compound as the most potent compound. At a concentration of 20 µg/mL, compound demonstrated a remarkable 99% inhibition of KYSE70 and KYSE150 cell growth after 48 h. IC was 0.655 µg/mL after 24 h. Additionally, potential anti-tumor cellular mechanisms were explored through molecular docking, which was used to predict the binding mode of with METAP2 and EGFR, suggesting that the C=O part of the pyridone moiety likely played a crucial role in binding. This study provided valuable insights and guidance for the development of novel anticancer drugs with novel structural scaffolds.

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