Bridged androstenediol analogs as ER-beta selective SERMs

Timothy A Blizzard; Candido Gude; Wanda Chan; Elizabeth T Birzin; Marina Mojena; Consuelo Tudela; Fang Chen; Kristin Knecht; Qin Su; Bryan Kraker; Mark A Holmes; Susan P Rohrer; Milton L Hammond

doi:10.1016/j.bmcl.2006.12.053

Bridged androstenediol analogs as ER-beta selective SERMs

Bioorg Med Chem Lett. 2007 May 15;17(10):2944-8. doi: 10.1016/j.bmcl.2006.12.053. Epub 2006 Dec 21.

Authors

Timothy A Blizzard¹, Candido Gude, Wanda Chan, Elizabeth T Birzin, Marina Mojena, Consuelo Tudela, Fang Chen, Kristin Knecht, Qin Su, Bryan Kraker, Mark A Holmes, Susan P Rohrer, Milton L Hammond

Affiliation

¹ Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com

PMID: 17448656
DOI: 10.1016/j.bmcl.2006.12.053

Abstract

A series of bridged androstenediol derivatives was prepared. The bridged compounds exhibited reduced ER-beta selectivity relative to uncyclized analogs.

MeSH terms

Androstenediols / chemical synthesis*
Androstenediols / pharmacology
Cyclization
Estrogen Receptor beta / antagonists & inhibitors*
Estrogen Receptor beta / chemistry
Estrogen Receptor beta / metabolism
Humans
Models, Molecular
Molecular Structure
Selective Estrogen Receptor Modulators / chemical synthesis*
Selective Estrogen Receptor Modulators / pharmacology*
Structure-Activity Relationship

Substances

Androstenediols
Estrogen Receptor beta
Selective Estrogen Receptor Modulators