Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/15716
Title: Flavonoid dimers as novel, potent antileishmanial agents
Authors: Wong, ILK
Chan, KF
Chan, TH
Chow, LMC 
Issue Date: 2012
Publisher: Amer Chemical Soc
Source: Journal of medicinal chemistry, 2012, v. 55, no. 20, p. 8891-8902 How to cite?
Journal: Journal of Medicinal Chemistry 
Abstract: The present study found that synthetic flavonoid dimers with either polyethylene glycol linker or amino ethyleneglycol linker have marked leishmanicidal activity. Compound 39 showed very consistent and promising leishmanicidal activity for both extracellular promastigotes (IC50 ranging from 0.13 to 0.21 μM) and intracellular amastigotes (IC50 = 0.63 μM) irrespective of the drug-sensitivity of parasites. Moreover, compound 39 displayed no toxicity toward macrophage RAW 264.7 cells (IC 50 > 100 μM) and primary mouse peritoneal elicited macrophages (IC50 > 88 μM). Its high value of therapeutic index (>140) was better than other highly potent antileishmanials such as amphotericin B (therapeutic index = 119). Compound 39 is therefore a new, safe, and effective antileishmanial candidate compound which is even effective against drug-refractory parasites.
URI: http://hdl.handle.net/10397/15716
DOI: 10.1021/jm301172v
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