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Synthesis and anti-HIV properties of new hydroxyquinoline-polyamine conjugates on cells infected by HIV-1 LAV and HIV-1 BaL viral strains.

Moret V, Dereudre-Bosquet N, Clayette P, Laras Y, Pietrancosta N, Rolland A, Weck C, Marc S, Kraus JL

Laboratoire de Chimie Biomoléculaire, UMR-CNRS 6216, IBDML, Université de la Méditerranée, Parc Scientifique de Luminy, case 901, 13288 Marseille cedex 9, France.

To find new derivatives that block different virus strains entry in cells bearing specific surface receptors represent an interesting challenge for medicinal chemists. Here, we report the synthesis and the anti-HIV properties of a new series of analogues based on the introduction of quinoline moiety on various polyamine backbones, including polyazamacrocycles. Three compounds 7, 8, and 10 of this series were found active on PBMCs cells infected by HIV-1 LAV or by HIV-1 BaL, in contrast the well-known reference compound 1a (AMD 3100) was found only active on HIV-1 LAV strain.

Published 10 November 2006 in Bioorg Med Chem Lett, 16(23): 5988-92.
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