title: The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
abstract: Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. robert_wilkening@merck.com
authors.forename: R R
authors.initials: RR
authors.lastname: Wilkening
authors.forename: R W
authors.initials: RW
authors.lastname: Ratcliffe
authors.forename: E C
authors.initials: EC
authors.lastname: Tynebor
authors.forename: K J
authors.initials: KJ
authors.lastname: Wildonger
authors.forename: A K
authors.initials: AK
authors.lastname: Fried
authors.forename: M L
authors.initials: ML
authors.lastname: Hammond
authors.forename: R T
authors.initials: RT
authors.lastname: Mosley
authors.forename: P M D
authors.initials: PM
authors.lastname: Fitzgerald
authors.forename: N
authors.initials: N
authors.lastname: Sharma
authors.forename: B M
authors.initials: BM
authors.lastname: McKeever
authors.forename: S
authors.initials: S
authors.lastname: Nilsson
authors.forename: M
authors.initials: M
authors.lastname: Carlquist
authors.forename: A
authors.initials: A
authors.lastname: Thorsell
authors.forename: L
authors.initials: L
authors.lastname: Locco
authors.forename: R
authors.initials: R
authors.lastname: Katz
authors.forename: K
authors.initials: K
authors.lastname: Frisch
authors.forename: E T
authors.initials: ET
authors.lastname: Birzin
authors.forename: H A
authors.initials: HA
authors.lastname: Wilkinson
authors.forename: S
authors.initials: S
authors.lastname: Mitra
authors.forename: S
authors.initials: S
authors.lastname: Cai
authors.forename: E C
authors.initials: EC
authors.lastname: Hayes
authors.forename: J M
authors.initials: JM
authors.lastname: Schaeffer
authors.forename: S P
authors.initials: SP
authors.lastname: Rohrer
mesh_terms: D002460:Cell Line; D018360:Crystallography, X-Ray; D047628:Estrogen Receptor alpha / Q000737:chemistry / Q000187:drug effects; D047629:Estrogen Receptor beta / Q000737:chemistry / Q000187:drug effects*; D005449:Fluorenes / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: C545987:4-bromo-9a-butyl-7-hydroxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005449:Fluorenes; D008024:Ligands