Synthesis and biological activity evaluation of hydrazone derivatives based on a Troger's base skeleton

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F15%3A43899958" target="_blank" >RIV/60461373:22340/15:43899958 - isvavai.cz</a>
Alternative codes found
RIV/68378050:_____/15:00455810 RIV/61989592:15110/15:33154138
Result on the web
<a href="http://dx.doi.org/10.1016/j.bmc.2015.01.029" target="_blank" >http://dx.doi.org/10.1016/j.bmc.2015.01.029</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2015.01.029" target="_blank" >10.1016/j.bmc.2015.01.029</a>

Result language
angličtina
Original language name
Synthesis and biological activity evaluation of hydrazone derivatives based on a Troger's base skeleton
Original language description
We report the design and synthesis of novel anticancer agents based on bis-hydrazones separated by a rigid Troger's base skeleton. This novel approach combines a biologically active moiety (hydrazone) with this scaffold (Troger's base) to construct DNA intercalators. Evaluation of the anticancer activity of these agents using seven cancer cell lines and two healthy cell lines found that several derivatives had potent anticancer activity and excellent selectivity indexes toward cancer cells. The antimicrobial activities were tested on a set of thirteen bacterial stains, but the prepared compounds were not active. Complexation studies using biologically important metal ions demonstrated that these compounds are able to bind Cu2+, Fe3+, Co2+, Ni2+ and Zn2+. DNA intercalation studies showed that the compounds themselves do not interact with DNA, but their metallocomplexes do interact, most likely via intercalation into DNA.
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
CE - Biochemistry
OECD FORD branch
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Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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