title: Synthesis and anti-HIV properties of new hydroxyquinoline-polyamine conjugates on cells infected by HIV-1 LAV and HIV-1 BaL viral strains.
abstract: 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.
authors.affiliation: Laboratoire de Chimie Biomoléculaire, UMR-CNRS 6216, IBDML, Université de la Méditerranée, Parc Scientifique de Luminy, case 901, 13288 Marseille cedex 9, France.
authors.forename: Vincent
authors.initials: V
authors.lastname: Moret
authors.forename: Nathalie
authors.initials: N
authors.lastname: Dereudre-Bosquet
authors.forename: Pascal
authors.initials: P
authors.lastname: Clayette
authors.forename: Younes
authors.initials: Y
authors.lastname: Laras
authors.forename: Nicolas
authors.initials: N
authors.lastname: Pietrancosta
authors.forename: Amandine
authors.initials: A
authors.lastname: Rolland
authors.forename: Clement
authors.initials: C
authors.lastname: Weck
authors.forename: Sylvain
authors.initials: S
authors.lastname: Marc
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Kraus
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D006912:Hydroxyquinolines / Q000737:chemistry*; D015394:Molecular Structure; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D006912:Hydroxyquinolines; D011073:Polyamines