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

  • Arch Pharm Res. 2012 Jan;35(1):27-33. doi: 10.1007/s12272-012-0103-1.
Mozna H Khraiwesh  1 ,  Clarence M Lee ,  Yakini Brandy ,  Emmanuel S Akinboye ,  Solomon Berhe ,  Genelle Gittens ,  Muneer M Abbas ,  Franklin R Ampy ,  Mohammad Ashraf ,  Oladapo Bakare
Affiliations
  • 1. Department of Biology, Howard University, Washington DC 20059, USA.
PMID: 22297740 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 (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).

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