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

Abstract : The synthesis of a series of thirty-eight new modified dinucleotides and dinucleotide conjugate analogues of d-(5')ApC(3') 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.
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Yves Aubert, Marcel Chassignol, Victoria Roig, Gladys Mbemba, Julien Weiss, et al.. Synthesis and anti-HIV-1 integrase activity of modified dinucleotides. European Journal of Medicinal Chemistry, Elsevier, 2009, 44 (12), pp.5029-5044. ⟨10.1016/j.ejmech.2009.09.007⟩. ⟨hal-00521651⟩



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