Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents |
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Authors: | Ping Zhou Linsheng Huang Jie Zhou Bin Jiang Yanmei Zhao Xuehua Deng Qin Zhao Fei Li |
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Institution: | 1. Department of Hepatopancreatobiliary Surgery, Taihe Hospital, Hubei University of Medicine, Hubei, China;2. School of Pharmaceutical Sciences, Hubei University of Medicine, Hubei, China |
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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 tumor cell lines 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 1.0 μM. 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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Keywords: | Synthesis Quinolone Antiproliferative activity Apoptosis |
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