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À propos de : Depsides and Depsidones as Inhibitors of HIV-1 Integrase: Discovery of NovelInhibitors through 3D Database Searching        

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  • Depsides and Depsidones as Inhibitors of HIV-1 Integrase: Discovery of NovelInhibitors through 3D Database Searching
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  • Seventeen lichen acids comprising depsides, depsidones,and their synthetic derivatives havebeen examined for their inhibitory activity against HIV-1 integrase,and two pharmacophoresassociated with inhibition of this enzyme have been identified. Asearch of the NCI 3D databaseof approximately 200 000 structures yielded some 800 compounds whichcontain one or theother pharmacophore. Forty-two of these compounds were assayed forHIV-1 integraseinhibition, and of these, 27 had inhibitory IC50 values ofless than 100 μM; 15 were below 50μM. Several of these compounds were also examined for theiractivity against HIV-2 integraseand mammalian topoisomerase I.
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