Synthesis and evaluation of 17α-Arylestradiols as ligands for estrogen receptor α and β

Article abstract of DOI:10.1021/jm901898a

To identify novel estrogen receptor ligands a series of substituted 17α-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17α-ethynylestradiol with various 1,7-diynes in the presence of Wilkinsons catalysts [Rh(PPh₃)₃Cl]. 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 ERα/ERβ and different selectivity as a result of differing potencies for either ER.