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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

  • Czech description

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

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

  • 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