Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives

Mozna H. Khraiwesh, Clarence M. Lee, Yakini Brandy, Emmanuel S. Akinboye, Solomon Berhe, Genelle Gittens, Muneer M. Abbas, Franklin R. Ampy, Mohammad Ashraf, Oladapo Bakare

Research output: Contribution to journalArticlepeer-review

Abstract

The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC 50 = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from 0.7 μM to 6.1 μM (p < 0.05). Studies of the cytotoxic activities of these compounds on a Balb/C 3T3 mouse fibroblast cell line revealed that four of these compounds, IMDNQ1, IMDNQ2, IMDNQ3, and IMDNQ10 displayed selectivity indices of 60.25, 53.97, 31.83, and 275.3, respectively, rendering them significantly (p < 0.05) more selective in inhibiting the parasite growth than nifurtimox (selectivity index = 10.86).

Original languageEnglish (US)
Pages (from-to)27-33
Number of pages7
JournalArchives of Pharmacal Research
Volume35
Issue number1
DOIs
StatePublished - Jan 2012

Keywords

  • Chagas disease
  • Cytotoxicity
  • Epimastigotes
  • Fibroblasts
  • Imido-substituted 1,4-naphthoquinone
  • Trypanosoma cruzi

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery
  • Organic Chemistry

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