Tacrine derivatives as dual topoisomerase I and II catalytic inhibitors

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F15%3A00446307" target="_blank" >RIV/68081707:_____/15:00446307 - isvavai.cz</a>

Alternative codes found

RIV/00179906:_____/15:10293865

Result on the web

<a href="http://dx.doi.org/10.1016/j.bioorg.2015.03.002" target="_blank" >http://dx.doi.org/10.1016/j.bioorg.2015.03.002</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bioorg.2015.03.002" target="_blank" >10.1016/j.bioorg.2015.03.002</a>

Result language

angličtina

Original language name

Tacrine derivatives as dual topoisomerase I and II catalytic inhibitors

Original language description

This study examines the binding properties of a series of newly synthetized tacrine derivatives 1-4 and their anticancer effects. Spectroscopic techniques (UV-Vis, fluorescence spectroscopy, thermal denaturation, and linear spectropolarimetry) and viscometry were used to study DNA binding properties and to determine the types of DNA interaction with the studied derivatives. The binding constants for the complexes with DNA were obtained using UV-Vis spectroscopic titrations (K = 1.6 x 10(4)-4.0 x 10(5) M-1) and electrophoretic methods were used to determine the effect of the derivatives on topoisomerase I and II activity. Monotacrine derivative 1 showed evidence of topoisomerase I relaxation activity at a concentration of 30 x 10(-6) M, while bistacrinederivatives 2-4 produced a complete inhibition of topoisomerase I at a concentration of 5 x 10(-6) M. The biological activities of the derivatives were studied using MTT-assay and flow cytometric methods (detection of mitochondrial membr

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

BO - Biophysics

OECD FORD branch

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Project

<a href="/en/project/LD14019" target="_blank" >LD14019: Molecular and cellular pharmacology of new conjugated organometalic compound. Relations to development of anticancer drugs.</a><br>

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2015

Confidentiality

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

Name of the periodical

Bioorganic Chemistry

ISSN

0045-2068

e-ISSN

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Volume of the periodical

59

Issue of the periodical within the volume

APR2015

Country of publishing house

US - UNITED STATES

Number of pages

9

Pages from-to

168-176

UT code for WoS article

000352211900016

EID of the result in the Scopus database

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