title: Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
abstract: A series of 3-aryl-7-hydroxybenzoxazine analogues have been prepared and evaluated as ligands for the two estrogen receptor subtypes (ERalpha and ERbeta). From the radioligand binding assay, compounds with more than a 10-fold binding selectivity toward the ERbeta subtype have been identified. These compounds have also been shown to be potent full agonists in the functional assay by activation of ERE promoted transcription, with the best compound being 20-fold more potent than genistein.
authors.affiliation: Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. wu.yang@bms.com
authors.forename: Wu
authors.initials: W
authors.lastname: Yang
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Wang
authors.forename: Zhengping
authors.initials: Z
authors.lastname: Ma
authors.forename: Rajasree
authors.initials: R
authors.lastname: Golla
authors.forename: Terry
authors.initials: T
authors.lastname: Stouch
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Seethala
authors.forename: Susan
authors.initials: S
authors.lastname: Johnson
authors.forename: Rong
authors.initials: R
authors.lastname: Zhou
authors.forename: Timur
authors.initials: T
authors.lastname: Güngör
authors.forename: Jean H M
authors.initials: JH
authors.lastname: Feyen
authors.forename: John K
authors.initials: JK
authors.lastname: Dickson
mesh_terms: D048588:Benzoxazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047629:Estrogen Receptor beta / Q000819:agonists*; D055672:Static Electricity; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D048588:Benzoxazines; D047629:Estrogen Receptor beta