Synthesis and in vitro evaluation of 4-substituted furano[3, 2-c] tetrahydroquinolines as potential anti-cancer agents. (2nd September 2016)

• Record Type: Journal Article
• Authors: Chen, Can; Zingales, Sarah; Wang, Ting; Yuan, Mingyong; Wang, Dan; Cai, Lulu; Jiang, Qinglin
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 31:Number 5(2016:Oct.)
• Page Start: 853
• Page End: 858
• Publication Date: 2016-09-02
• Subjects: Antitumor activity -- apoptosis -- diastereoselectivity -- tetrahydroquinoline derivatives; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2015.1064120
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: A convenient and mild method for the synthesis of substituted furano [3, 2-c]tetrahydroquinoline derivatives was developed, using the multi-component Povarov reaction. Of the synthesized tetrahydroquinoline derivatives, compound10a displayed the greatest cellular proliferation inhibitory activities with IC50 values of 2.5–16.7 μmol/l. In addition, 10a induced murine C6 glioma cell apoptosis in a dose-dependent manner by up-regulating the expression of Bax, caspase-3, and caspase-9, and by down-regulating Bcl-2. Our findings suggest that these novel compounds have potential as therapeutic agents via inducing mitochondrial apoptosis.