Počet záznamů: 1  

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

  1. 1. 0422820 - UMG-J 2014 RIV CH eng J - Článek v odborném periodiku
    Sedlák, David - Eignerová, Barbara - Dračínský, Martin - Janoušek, Zbyněk - Bartůněk, Petr - Kotora, Martin
    Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta.
    Journal of Organometallic Chemistry. Roč. 747, 1.12.2013 (2013), s. 178-183. ISSN 0022-328X
    Grant CEP: GA MŠk(CZ) LC06070; GA MŠk(CZ) LC06077; GA MŠk LM2011022; GA ČR GA204/09/1905
    Institucionální podpora: RVO:68378050 ; RVO:61388963
    Klíčová slova: carborane * estradiol * metathesis * estrogen receptor * steroid ligand
    Kód oboru RIV: EB - Genetika a molekulární biologie
    Impakt faktor: 2.302, rok: 2013

    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.
    Trvalý link: http://hdl.handle.net/11104/0229015