Flavonoid dimers as novel, potent antileishmanial agents

Iris L K Wong, Kin Fai Chan, Tak Hang Chan, Ming Cheung Chow

Research output: Journal article publicationJournal articleAcademic researchpeer-review

27 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)8891-8902
Number of pages12
JournalJournal of Medicinal Chemistry
Volume55
Issue number20
DOIs
Publication statusPublished - 25 Oct 2012

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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