HIV-1 is an etiologic agent of the acquired immunodeficiency syndrome (AIDS) that belongs to the retroviridae viral family which is responsible for one the greatest human health crises of the 20 th century. The development of effective antiviral treatments is of utmost importance. In this context, the presence of several G4 motifs in the U3 promoter region of the HIV-1 long terminal repeat (LTR), in both the viral and proviral genome, have been reported and it has been hypothesized that targeting these dynamic G4 sequences with small molecules can lead to the regulation of viral transcription, which in turn will result in decreased viral production. However, despite its significance, there are relatively few examples of small molecules that can selectively target viral G4 sequences including HIV-1. 2 Results