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.
Aubert
Yves
Y
Centre de Biophysique Moléculaire CNRS UPR 4301, affiliated with the University of Orléans and with INSERM Rue Charles Sadron, 45071 Orléans Cedex 02, France.
Chassignol
Marcel
M
Roig
Victoria
V
Mbemba
Gladys
G
Weiss
Julien
J
Meudal
Hervé
H
Mouscadet
Jean-François
JF
Asseline
Ulysse
U
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