Antitrypanosomal activities and cytotoxicity of some novel imido-substituted 1,4-naphthoquinone derivatives.
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).
Department of Biology, Howard University, Washington DC 20059, USA.
Mozna H
MH
Khraiwesh
Clarence M
CM
Lee
Yakini
Y
Brandy
Emmanuel S
ES
Akinboye
Solomon
S
Berhe
Genelle
G
Gittens
Muneer M
MM
Abbas
Franklin R
FR
Ampy
Mohammad
M
Ashraf
Oladapo
O
Bakare
D000818:Animals; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008807:Mice, Inbred BALB C; D041681:NIH 3T3 Cells; D009285:Naphthoquinones / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D003603:Cytotoxins; D009285:Naphthoquinones; D014344:Trypanocidal Agents; C035342:1,4-naphthoquinone