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

0356112 - ÚMG 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. E-ISSN 1520-4804
Grant CEP: GA MŠMT(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