Synthesis and anti-HIV-1 integrase activity of modified dinucleotides

The synthesis of a series of thirty-eight new modified dinucleotides and dinucleotide conjugate analogues of d-5′ApC3′ is described. The inhibitory activity of these compounds toward HIV-1 integrase was examined in enzymatic assays using the natural dinucleotide as a reference. Among the compounds, a perylene-dinucleotide conjugate has shown a two micromolar anti-integrase activity due to the presence of both the intercalator and the dinucleotide.

Graphical abstractThirty eight analogues of the dinucleotide5′CA3′ were synthesized and evaluated for their inhibitory effect on the HIV-1 integrase in enzymatic assays.Figure optionsDownload full-size imageDownload as PowerPoint slide