Author/Authors :
Seongkon Kim، نويسنده , , Jane Wu، نويسنده , , Helen Y. Chen، نويسنده , , Elizabeth T. Birzin، نويسنده , , Wanda Chan، نويسنده , , Yi Tien Yang، نويسنده , , Lawrence Colwell، نويسنده , , Susan Li، نويسنده , , Johanna Dahllund، نويسنده , , Frank DiNinno، نويسنده , , Susan P. Rohrer، نويسنده , , James M. Schaeffer، نويسنده , , Milton L. Hammond، نويسنده ,
Abstract :
A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERα selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay.
Keywords :
Benzoxathiin , SERM , e-mail: seongkon_kim@merck.com , fax: +1-732-594-9556 , Estrogen.* Corresponding author. Tel.: +1-732-594-8439
