About: Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	A series of 17 alpha-(carboranylalkyl)estradiols was synthesized using cross-metathesis reaction of 17 alpha-allyl- and 17 alpha-vinylestradiols with allylcarboranes catalyzed by Hoveyda-Grubbs 2nd generation catalyst. The prepared estradiol derivatives were tested in the panel of cell-based reporter assays including all steroid receptors. The compounds mainly activated estrogen receptors alpha and beta and tended to be weakly selective for ER alpha. Besides ER alpha and ER beta, we have also detected a weak agonistic activity on AR and PR at micromolar concentrations. We didn't observe any antagonistic effect with the exception of two receptors: GR and MR which were inhibited with some of the tested ligands. However, the inhibition was detectable at concentrations exceeding by far those needed to activate estrogen receptors. (C) 2013 Elsevier B. V. All rights reserved. A series of 17 alpha-(carboranylalkyl)estradiols was synthesized using cross-metathesis reaction of 17 alpha-allyl- and 17 alpha-vinylestradiols with allylcarboranes catalyzed by Hoveyda-Grubbs 2nd generation catalyst. The prepared estradiol derivatives were tested in the panel of cell-based reporter assays including all steroid receptors. The compounds mainly activated estrogen receptors alpha and beta and tended to be weakly selective for ER alpha. Besides ER alpha and ER beta, we have also detected a weak agonistic activity on AR and PR at micromolar concentrations. We didn't observe any antagonistic effect with the exception of two receptors: GR and MR which were inhibited with some of the tested ligands. However, the inhibition was detectable at concentrations exceeding by far those needed to activate estrogen receptors. (C) 2013 Elsevier B. V. All rights reserved. (en)
Title	Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta (en)
skos:prefLabel	Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta (en)
skos:notation	RIV/68378050:_____/13:00422820!RIV14-GA0-68378050
http://linked.open...avai/predkladatel	Ústav molekulární genetiky AV ČR, v. v. i.
http://linked.open...avai/riv/aktivita	I P Z
http://linked.open...avai/riv/aktivity	I, P(GA204/09/1905), P(LC06077), P(LM2011022), Z(MSM0021620857)
http://linked.open...iv/cisloPeriodika	1.12.2013
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Bartůněk, Petr Sedlák, David
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav molekulární genetiky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	109480
http://linked.open...ai/riv/idVysledku	RIV/68378050:_____/13:00422820
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	carborane; estradiol; metathesis; estrogen receptor; steroid ligand (en)
http://linked.open.../riv/klicoveSlovo	estradiol steroid ligand carborane metathesis estrogen receptor
http://linked.open...odStatuVydavatele	CH - Švýcarská konfederace
http://linked.open...ontrolniKodProRIV	[C725DBF04566]
http://linked.open...i/riv/nazevZdroje	Journal of Organometallic Chemistry
http://linked.open...in/vavai/riv/obor	EB
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	CZ-OPENSCREEN: National Infrastructure for Chemical Biology Center of Chemical Genetics Disp3: A potential role in the self renewal and differentiation of neural stem cells
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	747
http://linked.open...iv/tvurceVysledku	Bartůněk, Petr Dračínský, Martin Kotora, Martin Sedlák, David Janoušek, Zbyněk Eignerová, Barbara
http://linked.open...ain/vavai/riv/wos	000326116500025
http://linked.open...n/vavai/riv/zamer	Nové molekulární systémy pro pokročilé aplikace prospěšné pro zdraví a šetrné k životnímu prostředí
issn	0022-328X
number of pages	6 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.jorganchem.2013.06.013

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