Cytotoxicity of novel trifluoromethylquinoline derivatives on human leukemia cells

This report is a comparative study of the in vitro cell-growth inhibitory a ctivity of six new trifluoromethylquinoline derivatives on human promyelocy tic 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 IC50 of 10+/- 2.5 muM, 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 la tter, the cell growth inhibitory activity of these compounds appears to be due their ability to bind to and intercalate DNA. (C) 2001 Elsevier Science B.V. All rights reserved.