title: Total synthesis of eryvarin H and its derivatives and their biological activity as ERRγ inverse agonist.
abstract: Total synthesis of eryvarin H and a biological investigation of its analogues as a potential inverse agonist of ERRγ are described here. Among the 13 analogues prepared by the modular synthetic route, eryvarin H and compound showed meaningful ERRγ inverse agonistic activities along with moderate selectivity over ERα and other nuclear receptors in the cell-based reporter gene assay.
authors.affiliation: Department of Chemistry, Seoul National University, Seoul, Korea. sbpark@snu.ac.kr.
authors.forename: Ja Young
authors.initials: JY
authors.lastname: Koo
authors.forename: Sangmi
authors.initials: S
authors.lastname: Oh
authors.forename: Seung-Rye
authors.initials: SR
authors.lastname: Cho
authors.forename: Minseob
authors.initials: M
authors.lastname: Koh
authors.forename: Won-Keun
authors.initials: WK
authors.lastname: Oh
authors.forename: Hueng-Sik
authors.initials: HS
authors.lastname: Choi
authors.forename: Seung Bum
authors.initials: SB
authors.lastname: Park
mesh_terms: D002867:Chromones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004895:Erythrina / Q000737:chemistry*; D047628:Estrogen Receptor alpha / Q000819:agonists / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D008958:Models, Molecular; D062105:Molecular Docking Simulation; D011960:Receptors, Estrogen / Q000819:agonists* / Q000378:metabolism
chemical_list: D002867:Chromones; D047628:Estrogen Receptor alpha; D011960:Receptors, Estrogen; C586955:eryvarin H; C425824:estrogen receptor gamma