Synthesis, structural characterization and biological evaluation of novel stilbene derivatives as potential antimalarial agents.
A series of benzamide-containing stilbene derivatives was synthesized through the incorporation of short basic side-chains in the B-ring hydroxy position of resveratrol. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum D10 strain, showing IC(50) values between 1.5 and 80 microM, while their cytotoxicity was assessed using an human myeloid leukemia (U-937) cell line. With a selectivity ratio of > 51.02, the most selective of these derivatives, 29, also had the most lowest cytotoxic activity of the series.
Jung
Mankil
M
Department of Chemistry, Yonsei University, Seoul 120-749, South Korea.
Park
Won-Hwan
WH
Jung
Jae-Chul
JC
Lim
Eunyoung
E
Lee
Yongnam
Y
Oh
Seikwan
S
Moon
Hyung-In
HI
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D020128:Inhibitory Concentration 50; D010963:Plasmodium falciparum / Q000187:drug effects; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000962:Antimalarials; D013267:Stilbenes