Počet záznamů: 1

Synthesis and evaluation of 17 alpha-arylestradiols as ligands for estrogen receptor alpha and beta

  1. 1.
    0356112 - UMG-J 2011 RIV US eng J - Článek v odborném periodiku
    Sedlák, David - Novák, P. - Kotora, Martin - Bartůněk, Petr
    Synthesis and evaluation of 17 alpha-arylestradiols as ligands for estrogen receptor alpha and beta.
    Journal of Medicinal Chemistry. Roč. 53, č. 10 (2010), s. 4290-4294 ISSN 0022-2623
    Grant CEP: GA MŠk(CZ) LC06077
    Výzkumný záměr: CEZ:AV0Z50520514; CEZ:AV0Z40550506
    Klíčová slova: human breast cancer * estradiol * analogs
    Kód oboru RIV: EB - Genetika a molekulární biologie
    Impakt faktor: 5.207, rok: 2010

    To identify novel estrogen receptor ligands a series of substituted 17 alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17 alpha-ethynylestradiol with various 1,7-diynes in the presence of Wilkinson's catalysts [Rh(PPH3)(3)Cl]. The compounds were subjected to competitive binding assays, cell-based luciferase reporter assays, and proliferation assays. These experiments confirmed their estrogenic character and revealed some interesting properties like mixed partial/full agonism for ER alpha/ER beta and different selectivity as a result of differing potencies for either ER.
    Trvalý link: http://hdl.handle.net/11104/0194724
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