Synthesis and HIV-1 integrase inhibitory activities of caffeic acid dimers derived from Salvia officinalis.
The synthesis of two caffeoyl-coumarin conjugates, derived from sagecoumarin, has been accomplished, starting from ferulic acid, isoferulic acid and sesamol. Both compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in 3'-end processing reaction but were less effective against HIV-1 replication in a single-round infection assay of HeLa-beta-gal-CD4+ cells.
Bailly
Fabrice
F
Laboratoire de Chimie Organique et Macromoléculaire, UMR CNRS 8009, Université des Sciences et Technologies de Lille I, 59655 Villeneuve d'Ascq, France. Fabrice.Bailly@univ-lille1.fr
Queffelec
Clémence
C
Mbemba
Gladys
G
Mouscadet
Jean-François
JF
Cotelle
Philippe
P
D002109:Caffeic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D003374:Coumarins / Q000737:chemistry; D019281:Dimerization; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D027543:Salvia officinalis / Q000737:chemistry*
D002109:Caffeic Acids; D003374:Coumarins; D019428:HIV Integrase Inhibitors; C030123:coumarin; D019427:HIV Integrase