کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1985950 | 1540234 | 2016 | 33 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
New spiro tria(thia)zolidineâ¿¿acridines as topoisomerase inhibitors, DNA binders and cytostatic compounds
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موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
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چکیده انگلیسی
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 0.93 ÿ 104 M⿿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 50 μM) was evaluated both 48 h and 72 h 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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Biological Macromolecules - Volume 86, May 2016, Pages 690-700
Journal: International Journal of Biological Macromolecules - Volume 86, May 2016, Pages 690-700
نویسندگان
Othman M. Salem, Mária Vilková, Jana JanoÄ¿ková, Rastislav Jendželovský, Peter FedoroÄ¿ko, Eva Žilecká, Jana KaÅ¡párková, Viktor Brabec, Ján Imrich, Mária Kožurková,