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')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.
Centre de Biophysique Moléculaire CNRS UPR 4301, affiliated with the University of Orléans and with INSERM Rue Charles Sadron, 45071 Orléans Cedex 02, France.
Yves
Y
Aubert
Marcel
M
Chassignol
Victoria
V
Roig
Gladys
G
Mbemba
Julien
J
Weiss
Hervé
H
Meudal
Jean-François
JF
Mouscadet
Ulysse
U
Asseline
D001681:Biological Assay; D015226:Dinucleoside Phosphates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D010569:Perylene / Q000737:chemistry
D015226:Dinucleoside Phosphates; D019428:HIV Integrase Inhibitors; D010569:Perylene