877868-68-3Relevant academic research and scientific papers
Synthesis and evaluation of 4-(substituted styryl/alkenyl)-3,5-bis(4- hydroxyphenyl)-isoxazoles as ligands for the estrogen receptor
Haddad, Terra,Gershman, Rachel,Dilis, Robert,Hanson, Robert N.,Labaree, David,Hochberg, Richard B.
, p. 5999 - 6003,5 (2012)
A series of 3,5-bis (4-hydroxyphenyl) isoxazoles bearing a styryl/alkyl vinyl group at the 4-position were prepared and evaluated as ligands for the estrogen receptor-alpha (ERα). The target compounds were prepared using the Suzuki reaction to couple an iodo-isoxazole intermediate with a series of styryl/alkenyl boronic acids, followed by O-demethylation. The products were evaluated for their estrogen receptor-α ligand binding domain (ERα-LBD) binding affinity using a competitive binding assay. The 4-(4-hydroxystyryl) derivative 4 h displays binding properties similar to those of the previously described pyrazole class of ER ligands, indicating that the ERα-LBD tolerates the presence of the added vinyl group at the 4-position of the isoxazole ring.
