title: Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.
abstract: Several tetrahydrofluorenones with a triazole fused across C7-C8 showed high levels of ERbeta-selectivity and were found to be potent ERbeta-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERbeta.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. dann_parker@merck.com
authors.forename: Dann L
authors.initials: DL
authors.lastname: Parker
authors.forename: Dongfang
authors.initials: D
authors.lastname: Meng
authors.forename: Ronald W
authors.initials: RW
authors.lastname: Ratcliffe
authors.forename: Robert R
authors.initials: RR
authors.lastname: Wilkening
authors.forename: Donald M
authors.initials: DM
authors.lastname: Sperbeck
authors.forename: Mark L
authors.initials: ML
authors.lastname: Greenlee
authors.forename: Lawrence F
authors.initials: LF
authors.lastname: Colwell
authors.forename: Sherrie
authors.initials: S
authors.lastname: Lambert
authors.forename: Elizabeth T
authors.initials: ET
authors.lastname: Birzin
authors.forename: Katalin
authors.initials: K
authors.lastname: Frisch
authors.forename: Susan P
authors.initials: SP
authors.lastname: Rohrer
authors.forename: Stefan
authors.initials: S
authors.lastname: Nilsson
authors.forename: Ann-Gerd
authors.initials: AG
authors.lastname: Thorsell
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
mesh_terms: D000818:Animals; D001391:Azo Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D047629:Estrogen Receptor beta / Q000819:agonists* / Q000378:metabolism; D005449:Fluorenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D001391:Azo Compounds; D047629:Estrogen Receptor beta; D005449:Fluorenes; D008024:Ligands; C041509:fluorene