Bioorganic and medicinal chemistry letters p. 5999 - 6003,5 (2012)
Update date:2022-08-03
Topics:
Haddad, Terra
Gershman, Rachel
Dilis, Robert
Hanson, Robert N.
Labaree, David
Hochberg, Richard B.
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.
View MoreContact:+65 9658 0999
Address:26 Sin Ming Lane, Midview City, #05-118, Singapore 573971
Shanghai Witshoot Internet Technology Co Ltd
Contact:+86-21-66390020
Address:Room 419, No.285 Luochuan Road (E)
Lianyungang Ningkang Chemical Co., Ltd
Contact:.+86-518-88588008
Address:http://www.chemnk.com
Jinhua Haoyuan Chemical CO., LTD(expird)
Contact:86-579-82465583
Address:Jinhua,Zhejiang
Contact:+33-5-34012600
Address:28 ZA des Pignès
Doi:10.1021/ja00314a017
(1984)Doi:10.1021/jm00369a018
(1984)Doi:10.1016/S0040-4039(00)81796-7
(1983)Doi:10.1021/om050659j
(2006)Doi:10.1016/j.steroids.2017.09.013
(2017)Doi:10.1002/asia.202100173
(2021)