In this section, you can access to the latest technical information related to the FUTURE project topic.

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.

» Author: Ping Zhou, Linsheng Huang, Jie Zhou, Bin Jiang, Yanmei Zhao, Xuehua Deng, Qin Zhao, Fei Li

» Reference: Bioorganic & Medicinal Chemistry Letters, Volume 27, Issue 17

» Publication Date: 01/09/2017

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