Peet Julia, Selyutina Anastasia, Bredihhin Aleksei
Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
Bioorg Med Chem. 2016 Apr 15;24(8):1653-7. doi: 10.1016/j.bmc.2016.02.038. Epub 2016 Feb 28.
The antiretroviral activity of azulene derivatives was detected for the first time. A series of eighteen diversely substituted azulenes was synthesized and tested in vitro using HIV-1 based virus-like particles (VLPs) and infectious HIV-1 virus in U2OS and TZM-bl cell lines. Among the compounds tested, the 2-hydroxyazulenes demonstrated the most significant activity by inhibiting HIV-1 replication with IC50 of 2-10 and 8-20 μM for the VLPs and the infectious virus, respectively. These results indicate that azulene derivatives may be potentially useful candidates for the development of antiretroviral agents.
首次检测了薁衍生物的抗逆转录病毒活性。合成了一系列18种不同取代的薁，并在U2OS和TZM-bl细胞系中使用基于HIV-1的病毒样颗粒（VLP）和传染性HIV-1病毒进行体外测试。在所测试的化合物中，2-羟基薁表现出最显著的活性，对VLP和传染性病毒抑制HIV-1复制的IC50分别为2-10 μM和8-20 μM。这些结果表明，薁衍生物可能是开发抗逆转录病毒药物的潜在有用候选物。
