title: Aza analogues of equol: novel ligands for estrogen receptor beta.
abstract: 3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ERalpha and ERbeta. Several of these compounds exhibited binding selectivity for ER similar to that of genistein. Compounds 8c and 8d were found to have dual actions: antagonists for ERalpha and agonists for ERbeta in a yeast two-hybrid assay. These compounds have no estrogenic effects on the uterus and bone in vivo.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai, China.
authors.forename: Wuhong
authors.initials: W
authors.lastname: Chen
authors.forename: Zhaohu
authors.initials: Z
authors.lastname: Lin
authors.forename: Mengmeng
authors.initials: M
authors.lastname: Ning
authors.forename: Chunhao
authors.initials: C
authors.lastname: Yang
authors.forename: Xueming
authors.initials: X
authors.lastname: Yan
authors.forename: Yuyuan
authors.initials: Y
authors.lastname: Xie
authors.forename: Xu
authors.initials: X
authors.lastname: Shen
authors.forename: Ming-Wei
authors.initials: MW
authors.lastname: Wang
mesh_terms: D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015519:Bone Density; D060754:Equol; D047628:Estrogen Receptor alpha / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000378:metabolism*; D005260:Female; D006801:Humans; D007529:Isoflavones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D014599:Uterus / Q000187:drug effects
chemical_list: C007610:4',7-dihydroxy-3,4-dihydroisoflavone; D001372:Aza Compounds; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D007529:Isoflavones; D008024:Ligands; D060754:Equol