title: Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.
abstract: A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an ancillary aromatic ring linked by functionalized spacers such as amide, hydrazide, urea and 1-hydroxyprop-1-en-3-one moiety. Amide derivatives are the most promising ones and could serve as leads for further developments.
authors.affiliation: CNRS UMR 8076, Centre d'Etudes Pharmaceutiques, Chimie Organique, 5 rue J.-B. Clément, 92296 Châtenay-Malabry, France.
authors.forename: Christophe
authors.initials: C
authors.lastname: Bénard
authors.forename: Fatima
authors.initials: F
authors.lastname: Zouhiri
authors.forename: Marie
authors.initials: M
authors.lastname: Normand-Bayle
authors.forename: Michèle
authors.initials: M
authors.lastname: Danet
authors.forename: Didier
authors.initials: D
authors.lastname: Desmaële
authors.forename: Hervé
authors.initials: H
authors.lastname: Leh
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Mouscadet
authors.forename: Gladys
authors.initials: G
authors.lastname: Mbemba
authors.forename: Claire-Marie
authors.initials: CM
authors.lastname: Thomas
authors.forename: Sabine
authors.initials: S
authors.lastname: Bonnenfant
authors.forename: Marc
authors.initials: M
authors.lastname: Le Bret
authors.forename: Jean
authors.initials: J
authors.lastname: d'Angelo
mesh_terms: D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003432:Cross-Linking Reagents; D015658:HIV Infections / Q000188:drug therapy; D019427:HIV Integrase / Q000187:drug effects; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011804:Quinolines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014771:Virion / Q000187:drug effects
chemical_list: D003432:Cross-Linking Reagents; D019428:HIV Integrase Inhibitors; D011804:Quinolines; D019427:HIV Integrase