Structure activity relationship studies on cytotoxicity and the effects on steroid receptors of AB-functionalized cholestanes
The result's identifiers
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>
Alternative languages
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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Classification
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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Result continuities
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
Others
Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Steroid Biochemistry and Molecular Biology
ISSN
0960-0760
e-ISSN
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Volume of the periodical
159
Issue of the periodical within the volume
MAY
Country of publishing house
GB - UNITED KINGDOM
Number of pages
16
Pages from-to
154-169
UT code for WoS article
000374916500019
EID of the result in the Scopus database
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