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KMID : 0043320120350010027
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Archives of Pharmacal Research
2012 Volume.35 No. 1 p.27 ~ p.33
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Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives
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Khraiwesh Mozna H.
Berhe Solomon
Gittens Genelle
Abbas Muneer M.
Ashraf Mohammad
Bakare Oladapo
Lee Clarence M.
Brandy Yakini
Akinboye Emmanuel S.
Ampy Franklin R.
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Abstract
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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).
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KEYWORD
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Imido-substituted 1, 4-naphthoquinone, Trypanosoma cruzi, Cytotoxicity, Chagas disease, Epimastigotes, Fibroblasts
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