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Synthesis, Structural Characterization and Biological Evaluation of Novel Stilbene Derivatives as Potential Antimalarial Agents
Author(s) -
Jung Mankil,
Park WonHwan,
Jung JaeChul,
Lim Eunyoung,
Lee Yongnam,
Oh Seikwan,
Moon HyungIn
Publication year - 2009
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2009.00775.x
Subject(s) - plasmodium falciparum , cytotoxicity , chemistry , benzamide , stereochemistry , selectivity , resveratrol , in vitro , combinatorial chemistry , side chain , antimalarial agent , structure–activity relationship , cell culture , myeloid leukemia , biochemistry , biology , organic chemistry , cancer research , polymer , genetics , malaria , immunology , catalysis
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 μ m , 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.