Author/Authors :
Helen Y. Chen، نويسنده , , Seongkon Kim، نويسنده , , Jane Y. Wu، نويسنده , , Elizabeth T. Birzin، نويسنده , , Wanda Chan، نويسنده , , Yi Tien Yang، نويسنده , , Johanna Dahllund، نويسنده , , Frank DiNinno، نويسنده , , Susan P. Rohrer، نويسنده , , James M. Schaeffer، نويسنده , , Milton L. Hammond، نويسنده ,
Abstract :
A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ERα over ERβ, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.
Keywords :
Dihydrobenzoxathiin , SERMs , SERAMs.* Corresponding author. Tel.: +1-7325945323 , e-mail: helen_chen@merck.com , fax: +1-7325949556