Synthesis and Evaluation of 17α-Arylestradiols as Ligands for Estrogen Receptor α and β

Abstract

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 Wilkinson's catalysts [Rh(PPh3)3Cl].

Keywords

• 17α-arylestradiols
• ligands
• estrogen receptor
• human breast cancer
• estradiol
• analogs