. "Janou\u0161ek, Zbyn\u011Bk" . "[C725DBF04566]" . "747" . "CH - \u0160v\u00FDcarsk\u00E1 konfederace" . "000326116500025" . . . "carborane; estradiol; metathesis; estrogen receptor; steroid ligand"@en . . "2"^^ . . "Journal of Organometallic Chemistry" . . . . . . "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 . . "RIV/68378050:_____/13:00422820!RIV14-GA0-68378050" . "RIV/68378050:_____/13:00422820" . . "6"^^ . . . "Dra\u010D\u00EDnsk\u00FD, Martin" . . . "I, P(GA204/09/1905), P(LC06077), P(LM2011022), Z(MSM0021620857)" . "Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta"@en . "0022-328X" . "Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta"@en . "1.12.2013" . . . "Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta" . "Bart\u016Fn\u011Bk, Petr" . . "10.1016/j.jorganchem.2013.06.013" . "109480" . "Synthesis and evaluation of 17 alpha-(carboranylalkyl)estradiols as ligands for estrogen receptors alpha and beta" . "6"^^ . "Sedl\u00E1k, David" . "Eignerov\u00E1, Barbara" . . "Kotora, Martin" . . . . "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." . .