New spiro tria(thia)zolidine⿿acridines as topoisomerase inhibitors, DNA binders and cytostatic compounds
2016
Salem, Othman M. | Vilková, Mária | JanoĿková, Jana | Jendželovský, Rastislav | FedoroĿko, Peter | Žilecká, Eva | Kašpárková, Jana | Brabec, V. (Viktor) | Imrich, Ján | Kožurková, Mária
Three new diphenylsubstituted spirotriazolidine- and thiazolidinone⿿acridines were prepared and their interaction with calf thymus DNA investigated with UV⿿vis, fluorescence, circular dichroism spectroscopy and viscometry. The binding constants K were estimated to range from 0.34 to 0.93ÿ104M⿿1. UV⿿vis, fluorescence and circular dichroism measurements indicated that the compounds act as effective DNA-interacting agents. Electrophoretic separation proved that ligands inhibited topoisomerase I and II. The biological activity of compounds 3, 5 &6 at several different concentrations (10, 20 and 50μM) was evaluated both 48h and 72h following their addition to HL-60 cancer cells. The results were analysed using various different techniques (MMP detection, changes in metabolic activity/viability and analysis of cell cycle distribution). Acridine was also used as the positive control in these assays. The results from MMP analysis demonstrate the strong effect of 3-diphenylamino-2-(acridin-9-yl)imino-1,3-thiazolidin-4-one (5) on mitochondrial physiology. Cell viability analysis showed that acridine derivatives 3 and 6 were less effective than derivative 5 and the acridine control.
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