Ten dibenzofurans were synthesized and evaluated as human immunodeficiency virus (HIV)-1 inhibitors in vitro for the first time. Among these compounds, compounds 1, 6, 7 and 8 demonstrated significant anti-HIV-1 activity. Especially compound 1 showed the highest anti-HIV-1 activity with TI value larger than 16.18. Meanwhile, some structureactivity relationships were also observed and will provide a new lead for design and discovery of more potent dibenzofurans as new HIV-1 inhibitors.
Keywords: Dibenzofuran, Human immunodeficiency virus, Inhibitor, Synthesis