Synthesis and In Vitro Evaluation of 4-Substituted Furano[3,2-c] Tetrahydroquinolines as Potential Anti-Cancer Agents
Journal of Enzyme Inhibition and Medicinal Chemistry
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, compound 10a 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.
Chen, Can, Sarah Zingales, Ting Wang, Mingyong Yuan, Dan Wang, Lulu Cai, Qinglin Jiang.
"Synthesis and In Vitro Evaluation of 4-Substituted Furano[3,2-c] Tetrahydroquinolines as Potential Anti-Cancer Agents."
Journal of Enzyme Inhibition and Medicinal Chemistry, 31 (5): 853-858: Taylor & Francis Online.