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Androstene-3,5-dienes as ER-beta selective SERMs.

Bioorganic & medicinal chemistry letters (2007-09-25)
Timothy A Blizzard, Candido Gude, Jerry D Morgan, Wanda Chan, Elizabeth T Birzin, Marina Mojena, Consuelo Tudela, Fang Chen, Kristin Knecht, Qin Su, Bryan Kraker, Ralph T Mosley, Mark A Holmes, Susan P Rohrer, Milton L Hammond
ABSTRACT

A series of androstene-3,5-diene derivatives were prepared. Despite lacking the C-3 hydroxyl previously believed necessary for ER activity, some of the analogs retained surprising affinity for ER-beta. For example, diene 4 retained excellent selectivity and potency as an ER-beta agonist and was more selective for ER-beta over the androgen receptor (AR).

MATERIALS
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