New spiro tria(thia)zolidine-acridines as topoisomerase inhibitors, DNA binders and cytostatic compounds

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F16%3A10323437" target="_blank" >RIV/00179906:_____/16:10323437 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/16:33161173
Result on the web
<a href="http://dx.doi.org/10.1016/j.ijbiomac.2016.02.018" target="_blank" >http://dx.doi.org/10.1016/j.ijbiomac.2016.02.018</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ijbiomac.2016.02.018" target="_blank" >10.1016/j.ijbiomac.2016.02.018</a>

Result language
angličtina
Original language name
New spiro tria(thia)zolidine-acridines as topoisomerase inhibitors, DNA binders and cytostatic compounds
Original language description
tThree new diphenylsubstituted spirotriazolidine- and thiazolidinone-acridines were prepared and theirinteraction with calf thymus DNA investigated with UV-vis, fluorescence, circular dichroism spectroscopyand viscometry. The binding constants K were estimated to range from 0.34 to 0.93 x 104M -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. Thebiological activity of compounds 3, 5 & 6 at several different concentrations (10, 20 and 50 M) wasevaluated both 48 h and 72 h following their addition to HL-60 cancer cells. The results were analysedusing various different techniques (MMP detection, changes in metabolic activity/viability and analysisof cell cycle distribution). Acridine was also used as the positive control in these assays. The results fromMMP 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 6were less effective than derivative 5 and the acridine control.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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