Author/Authors :
Jian Liu، نويسنده , , Elizabeth T. Birzin، نويسنده , , Wanda Chan، نويسنده , , Yi Tien Yang، نويسنده , , Lee-Yuh Pai، نويسنده , , Carolyn DaSilva، نويسنده , , Edward C. Hayes، نويسنده , , Ralph T. Mosley، نويسنده , , Frank DiNinno، نويسنده , , Susan P. Rohrer، نويسنده , , James M. Schaeffer، نويسنده , , Milton L. Hammond، نويسنده ,
Abstract :
The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERα selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochroman and isothiochroman compounds were found to exhibit equipotent binding affinities to the ER isoforms and were less active in the inhibition of estradiol-triggered uterine growth when compared to I and lasofoxifene.
Keywords :
Isothiochroman , SERMs , Estrogen receptors , Isochroman
