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.

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