Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.
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.
Bénard
Christophe
C
CNRS UMR 8076, Centre d'Etudes Pharmaceutiques, Chimie Organique, 5 rue J.-B. Clément, 92296 Châtenay-Malabry, France.
Zouhiri
Fatima
F
Normand-Bayle
Marie
M
Danet
Michèle
M
Desmaële
Didier
D
Leh
Hervé
H
Mouscadet
Jean-François
JF
Mbemba
Gladys
G
Thomas
Claire-Marie
CM
Bonnenfant
Sabine
S
Le Bret
Marc
M
d'Angelo
Jean
J
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
D003432:Cross-Linking Reagents; D019428:HIV Integrase Inhibitors; D011804:Quinolines; D019427:HIV Integrase