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Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. Epub 2007 Sep 7.

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

Author information

1
Merck Research Laboratories, Rahway, NJ 07065, USA. tim_blizzard@merck.com

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).

PMID:
17890084
DOI:
10.1016/j.bmcl.2007.09.001
[Indexed for MEDLINE]

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