Synthesis and in vitro evaluation of 4-substituted furano[3,2-c] tetrahydroquinolines as potential anti-cancer agents.
作者信息
Chen Can, Zingales Sarah, Wang Ting, Yuan Mingyong, Wang Dan, Cai Lulu, Jiang Qinglin
机构信息
a College of Pharmacy and the First Affiliated Hospital, Chengdu Medical College , Chengdu , PR China .
b Department of Pharmacy , Sichuan Provincial People's Hospital , Chengdu , PR China .
出版信息
J Enzyme Inhib Med Chem. 2016 Oct;31(5):853-8. doi: 10.3109/14756366.2015.1064120. Epub 2015 Jul 24.
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.
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