Androstenediol analogs as ER-beta-selective SERMs

Timothy A Blizzard; Candido Gude; Jerry D Morgan 2nd; Wanda Chan; Elizabeth T Birzin; Marina Mojena; Consuelo Tudela; Fang Chen; Kristin Knecht; Qin Su; Bryan Kraker; Ralph T Mosley; Mark A Holmes; Nandini Sharma; Paula M D Fitzgerald; Susan P Rohrer; Milton L Hammond

doi:10.1016/j.bmcl.2005.11.014

Androstenediol analogs as ER-beta-selective SERMs

Bioorg Med Chem Lett. 2006 Feb 15;16(4):834-8. doi: 10.1016/j.bmcl.2005.11.014. Epub 2005 Nov 23.

Authors

Timothy A Blizzard¹, Candido Gude, Jerry D Morgan 2nd, Wanda Chan, Elizabeth T Birzin, Marina Mojena, Consuelo Tudela, Fang Chen, Kristin Knecht, Qin Su, Bryan Kraker, Ralph T Mosley, Mark A Holmes, Nandini Sharma, Paula M D Fitzgerald, Susan P Rohrer, Milton L Hammond

Affiliation

¹ Merck Research Laboratories, PO Box 2000, Rahway NJ 07065, USA. [email protected]

PMID: 16309907
DOI: 10.1016/j.bmcl.2005.11.014

Abstract

A series of 19-substituted androstenediol derivatives was prepared. Some of the novel analogs were surprisingly potent and selective ligands for ER-beta.

MeSH terms

Androstenediol / analogs & derivatives*
Androstenediol / chemical synthesis
Androstenediol / pharmacology*
Crystallography, X-Ray
Estrogen Receptor beta / drug effects*
Humans
Ligands
Models, Molecular
Molecular Conformation
Selective Estrogen Receptor Modulators / chemical synthesis
Selective Estrogen Receptor Modulators / pharmacology*
Stereoisomerism
Structure-Activity Relationship

Substances

Estrogen Receptor beta
Ligands
Selective Estrogen Receptor Modulators
Androstenediol