Anti-HIV and antiplasmodial activity of original flavonoid derivatives.
In our search for potent anti-HIV and antiplasmodial agents, novel series of flavonoid derivatives and their chalcone intermediates were synthesized and evaluated for inhibition of HIV multiplication and antiproliferative activity on Plasmodium falciparum parasites. Chalcones exhibited a more selective antiplasmodial activity than flavonoids. Methoxyflavone 7e was the only one compound active in both P. falciparum and HIV-1 whereas aminomethoxyflavones showed activity against HIV-2. Para substitution on the B ring seemed to increase HIV-2 potency.
Casano
Gilles
G
Aix-Marseille Université, Institut des Sciences Moléculaires de Marseille, iSm2-UMR CNRS, Centre Saint Jérôme, Marseille Cedex 20, France.
Dumètre
Aurélien
A
Pannecouque
Christophe
C
Hutter
Sébastien
S
Azas
Nadine
N
Robin
Maxime
M
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006678:HIV / Q000187:drug effects; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects
D019380:Anti-HIV Agents; D000962:Antimalarials; D005419:Flavonoids