Archives of Pharmacal Research

, Volume 35, Issue 1, pp 27–33

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 Article Drug Design and Discovery

DOI: 10.1007/s12272-012-0103-1

Cite this article as:
Khraiwesh, M.H., Lee, C.M., Brandy, Y. et al. Arch. Pharm. Res. (2012) 35: 27. doi:10.1007/s12272-012-0103-1

Abstract

The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC50 = 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).

Key words

Imido-substituted 1,4-naphthoquinoneTrypanosoma cruziCytotoxicityChagas diseaseEpimastigotesFibroblasts

Copyright information

© The Pharmaceutical Society of Korea and Springer Netherlands 2012

Authors and Affiliations

  • Mozna H. Khraiwesh
    • 1
  • Clarence M. Lee
    • 1
  • Yakini Brandy
    • 2
  • Emmanuel S. Akinboye
    • 2
  • Solomon Berhe
    • 2
  • Genelle Gittens
    • 2
  • Muneer M. Abbas
    • 3
  • Franklin R. Ampy
    • 1
  • Mohammad Ashraf
    • 4
  • Oladapo Bakare
    • 2
  1. 1.Department of BiologyHoward UniversityWashington DCUSA
  2. 2.Department of ChemistryHoward UniversityWashington DCUSA
  3. 3.College of Medicine, The National Human Genome CenterHoward UniversityWashington DCUSA
  4. 4.Department of Comprehensive SciencesHoward UniversityWashington DCUSA