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

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/61989592:15310/16:33161173

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2016

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

International Journal of Biological Macromolecules

ISSN

0141-8130

e-ISSN

—

Svazek periodika

86

Číslo periodika v rámci svazku

May

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

11

Strana od-do

690-700

Kód UT WoS článku

000374196100081

EID výsledku v databázi Scopus

2-s2.0-84957837082