Bioorganic & Medicinal Chemistry Letters 2003-12-15

B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens.

Charles W Lugar, David Magee, Mary D Adrian, Pamela Shetler, Henry U Bryant, Jeffrey A Dodge

Index: Bioorg. Med. Chem. Lett. 13(24) , 4281-4, (2003)

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Abstract

The pharmacology and SAR of representative equine estogens is described. 17alpha-Dihydroequilenin was found to prevent bone loss after 5 weeks of oral administration to ovariectomized rats. The stereochemical significance of the D-ring and the C/D ring juncture was investigated with a series of benzothiophene-based equilenin analogues.

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