In Vitro Antiplasmodial Activity and Cytotoxic Effect of (Z)-2-Benzylidene-4, 6-Dimethoxybenzofuran-3(2H)-One Derivatives.

BACKGROUND

Aurones are naturally occurring compounds that belong to flavenoids family and have antiplasmodial effects. This study investigated some new aurones derivatives against chloroquine sensitive Plasmodium falciparum. Here we report the synthesis, in vitro antiplasmodial activity and cytotoxic evaluation of 11 compound from derivatives of (Z)-2- benzylidene-4, 6-dimethoxybenzofuran-3(2H)-one.

METHODS

The cytotoxic evaluations of active compounds were performed with MTT (3-[4, 5-dimethylthiazol-2-yl]-2, 5 diphenyltetrazolium bromide) assay on human breast cancer cell lines; MCF7 and T47D.

RESULTS

From 11 compounds M3, M6 and M7 compounds showed good anti-plasmodial effect against chloroquine-sensitive 3D strain of P. falciparum with IC50 (50% inhibitory concentration) values of 7.82, 7.27 and 2.3 μM respectively. No noticeable toxicity was observed with these compounds when tested against tested cell lines.

CONCLUSION

The replacement of the 4 and 5 positions at ring B of aurone derivatives, with propoxy and bromide (Br) respectively was revealed highly advantageous for their antiplasmodial effect.