作者:Julia Peet、Anastasia Selyutina、Aleksei Bredihhin
DOI:10.1016/j.bmc.2016.02.038
日期:2016.4
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
首次检测到z烯衍生物的抗逆转录病毒活性。使用基于HIV-1的病毒样颗粒(VLP)和感染性HIV-1病毒在U2OS和TZM-bl细胞系中合成了一系列十八种不同取代的天青石,并在体外进行了测试。在所测试的化合物中,2-羟基az烯酮通过抑制HIV-1复制而表现出最显着的活性,对VLP和传染性病毒的IC 50分别为2-10和8-20μM。这些结果表明,z唑衍生物可能是开发抗逆转录病毒药物的潜在有用候选物。