Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
4 years ago

Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents

Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents
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.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X1730700X

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