title: Androstene-3,5-dienes as ER-beta selective SERMs.
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).
authors: Merck Research Laboratories, Rahway, NJ 07065, USA. tim_blizzard@merck.com
authors: Timothy A
authors: TA
authors: Blizzard
authors: Candido
authors: C
authors: Gude
authors: Jerry D
authors: JD
authors: Morgan
authors: Wanda
authors: W
authors: Chan
authors: Elizabeth T
authors: ET
authors: Birzin
authors: Marina
authors: M
authors: Mojena
authors: Consuelo
authors: C
authors: Tudela
authors: Fang
authors: F
authors: Chen
authors: Kristin
authors: K
authors: Knecht
authors: Qin
authors: Q
authors: Su
authors: Bryan
authors: B
authors: Kraker
authors: Ralph T
authors: RT
authors: Mosley
authors: Mark A
authors: MA
authors: Holmes
authors: Susan P
authors: SP
authors: Rohrer
authors: Milton L
authors: ML
authors: Hammond
mesh_terms: D000730:Androstadienes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D018360:Crystallography, X-Ray; D047629:Estrogen Receptor beta / Q000819:agonists*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D051381:Rats; D011944:Receptors, Androgen / Q000187:drug effects; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000730:Androstadienes; D047629:Estrogen Receptor beta; D011944:Receptors, Androgen; D020845:Selective Estrogen Receptor Modulators