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 IC₅₀ values between 1.5 and 80 μm, 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.