Structure activity relationship studies on cytotoxicity and the effects on steroid receptors of AB-functionalized cholestanes

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F16%3A00461520" target="_blank" >RIV/61389030:_____/16:00461520 - isvavai.cz</a>
Alternative codes found
RIV/68378050:_____/16:00461520 RIV/61388963:_____/16:00461520 RIV/61989592:15310/16:33161810 RIV/61989592:15110/16:33161810
Result on the web
<a href="http://dx.doi.org/10.1016/j.jsbmb.2016.03.017" target="_blank" >http://dx.doi.org/10.1016/j.jsbmb.2016.03.017</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.jsbmb.2016.03.017" target="_blank" >10.1016/j.jsbmb.2016.03.017</a>

Result language
angličtina
Original language name
Structure activity relationship studies on cytotoxicity and the effects on steroid receptors of AB-functionalized cholestanes
Original language description
Structure-activity relationship analysis and profiling of a library of AB-functionalized cholestane derivatives closely related to brassinosteroids (BRs) were performed to examine their antiproliferative activities and activities on steroid hormone receptors. Some of the compounds were found to have strong cytotoxic activity in several human normal and cancer cell lines. The presence of a 3-hydroxy or 3-oxo group and 2,3-vicinal diol or 3,4-vicinal diol moiety were found to be necessary for optimum biological activity, as well as a six-membered B ring. According to the profiling of all steroid receptors in both agonist and antagonist mode, the majority of the cholestanes were weakly active or inactive compared to the natural ligands. Estrogenic activity was detected for two compounds, two compounds possessed antagonistic properties on estrogen receptors and seven compounds showed agonistic activity. Two active cholestane derivatives were shown to strongly influence cell viability, proliferation, cell cycle distribution, apoptosis and molecular pathways responsible for these processes in hormone-sensitive/insensitive (MCF7/MDA-MB-468) breast cancer cell lines.
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
EB - Genetics and molecular biology
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
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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