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Updated: Feb 25, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents
Ping Zhou1, Linsheng Huang1, Jie Zhou2
1Department of Hepatopancreatobiliary Surgery, Taihe Hospital, Hubei University of Medicine, Hubei, China.
Abstract:
A series of novel 4(1H)-quinolone derivatives was synthesized and evaluated for antiproliferative activity in vitro. The results showed that these compounds exhibited more potent antiproliferative effect against a panel of human tumorcelllines than the lead compound 7-chloro-4(1H)-quinolone 1. Compound 7e was found to be the most potent antiproliferative agent and to exhibit selective cytotoxic activity against HepG2 cell lines with IC50 value lower than 1.0μM. Annexin V/FITC-PI assay showed that compound 7e induced apoptosis in HepG2 cells with a dose-dependent manner. Western blotting analysis indicated that compound 7e induced cell cycle arrest in G2/M phase by p53-depedent pathway.
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