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Synthesis,Structural Characterization and Biological Evaluation of Novel Stilbene Derivatives as Potential Antimalarial Agents
Authors:Mankil Jung  Won‐Hwan Park  Jae‐Chul Jung  Eunyoung Lim  Yongnam Lee  Seikwan Oh  Hyung‐In Moon
Affiliation:1. Department of Chemistry, Yonsei University, Seoul 120‐749, South Korea;2. Department of Diagnostics, College of Korean Medicine and Cardiovascular Medical Research Center, Dongguk University, Gyeong‐Ju 780‐714, South Korea;3. These authors equally contributed to this work;4. Department of Neuroscience and Medical Research Institute, School of Medicine, Ewha Womans University, Seoul 158‐710, South Korea;5. Department of Neuroscience and Inam Neuroscience Research Center, Sanbon Medical Center, Wonkwang University, Kyunggido 435‐040, South Korea
Abstract:
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.
Keywords:antiplasmodial activity  Plasmodium falciparum  resveratrol  selectivity ratio  stilbene derivatives
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