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.
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