Synthesis and in vitro evaluation of 4-substituted furano[3,2-c]tetrahydroquinolines as potential anti-cancer agents
Synthesis and in vitro evaluation of 4-substituted furano[3,2-c]tetrahydroquinolines as potential anti-cancer agents
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DOI：
10.3109/14756366.2015.1064120
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发表时间：
2016-01-01
影响因子：
5.6
通讯作者：
Jiang, Qinglin
中科院分区：
文献类型：
--
作者：
Chen, Can;Zingales, Sarah;Jiang, Qinglin
利用多组分Povarov反应，发展了一种简便、温和的合成取代呋喃并[3，2-c]四氢喹啉衍生物的方法。在合成的四氢喹啉衍生物中，化合物10a显示出最大的细胞增殖抑制活性，IC 50值为2.5-16.7 μ mol/l。此外，10a通过上调Bax、半胱天冬酶-3和半胱天冬酶-9的表达以及通过下调Bcl-2以剂量依赖性方式诱导鼠C6胶质瘤细胞凋亡。我们的研究结果表明，这些新的化合物有潜力作为治疗剂，通过诱导线粒体凋亡。
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 mu mol/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.