Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents. Issue 17 (1st September 2017)

• Record Type: Journal Article
• Authors: Zhou, Ping; Huang, Linsheng; Zhou, Jie; Jiang, Bin; Zhao, Yanmei; Deng, Xuehua; Zhao, Qin; Li, Fei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 17(2017)
• Page Start: 4185
• Page End: 4189
• Publication Date: 2017-09-01
• Subjects: Synthesis -- Quinolone -- Antiproliferative activity -- Apoptosis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.07.005
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: The representative compound7e could induce apoptosis in HepG2 cells with a dose-dependent manner and cell cycle arrest in G2/M phase by p53-depedent pathway. Abstract: A series of novel 4(1 H )-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(1 H )-quinolone1 . Compound7e 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 compound7e induced apoptosis in HepG2 cells with a dose-dependent manner. Western blotting analysis indicated that compound7e induced cell cycle arrest in G2/M phase by p53-depedent pathway.