School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1107-10. doi: 10.1016/j.bmcl.2011.11.121. Epub 2011 Dec 4.
Hepatitis C virus (HCV) infection is a main cause of chronic liver disease, leading to liver cirrhosis and hepatocellular carcinoma (HCC). The objective of our research was to develop effective agents against viral replication. Here, we have synthesized a series of anilinoquinoline derivatives. Based on a cell-based HCV replicon system, we observed that 2-(3'-nitroanilino)quinoline (18) exhibited anti-HCV activity with a 50% effective concentration (EC(50)) value of 7μM and a selective index (SI) value of 10. In addition, compound 18 possessed the inhibitory effect on HCV NS3/4A protease activity. Therefore, we concluded that the compound 18 possessed a potent activity against HCV replication and could provide as a new lead compound as anti-HCV inhibitor.
丙型肝炎病毒（HCV）感染是慢性肝病的主要病因，可导致肝硬化和肝细胞癌（HCC）。我们的研究目的是开发针对病毒复制的有效药物。在这里，我们合成了一系列的苯胺基喹啉衍生物。基于基于细胞的 HCV 复制子系统，我们观察到 2-(3'-硝基苯胺基)喹啉（18）对 HCV 表现出抗病毒活性，其 50%有效浓度（EC(50)）值为 7μM，选择性指数（SI）值为 10。此外，化合物 18 对 HCV NS3/4A 蛋白酶活性具有抑制作用。因此，我们得出结论，化合物 18 对 HCV 复制具有很强的活性，可以作为新型抗 HCV 抑制剂的先导化合物。
