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Updated: Oct 9, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Cytotoxicity of novel trifluoromethylquinoline derivatives on human leukemia cells
1Department of Pharmaceutical Chemistry, University of the North, Private Bag X1106, Sovenga 0717, South Africa. kgokongj@unin.unorth.ac.za
Abstract:
This report is a comparative study of the in vitro cell-growth inhibitory activity of six new trifluoromethylquinoline derivatives on human promyelocytic leukemic cells and the evaluation of their DNA binding characteristics. 2,8-Bis(trifluoromethyl)quinoline-4-(N(4)-ethyl-5-nitroimidazolo)methylene ketone shows the highest cell-growth inhibitory activity with IC(50) of 10+/-2.5 microM, causes extensive changes in the morphology of the HL-60 cells and appears to induce apoptosis. The other compounds are only moderately growth-inhibitory, while 8-trifluoromethylquinoline-4-(N(4)-ethyl-5-nitroimidazolo)methylene ketone is actually stimulatory to cell growth. Except for the latter, the cell growth inhibitory activity of these compounds appears to be due their ability to bind to and intercalate DNA.
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