title: Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
abstract: A novel SERM (selective estrogen receptor modulators), 1-(R), a chromene-derived bisbenzopyran, was discovered to alleviate hot flushes and effectively increase vaginal fluidity in rats. Moreover, 1-(R) was found to have beneficial effects on plasma cholesterol and bone metabolism while maintaining antiestrogenic activity in the uterus. The biological profile of its enantiomer 1-(S) was also evaluated.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development LLC, 1000 Route 202, Raritan, New Jersey 08869, USA.
authors.forename: Nareshkumar
authors.initials: N
authors.lastname: Jain
authors.forename: Ramesh M
authors.initials: RM
authors.lastname: Kanojia
authors.forename: Jiayi
authors.initials: J
authors.lastname: Xu
authors.forename: Guo
authors.initials: G
authors.lastname: Jian-Zhong
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Pacia
authors.forename: Muh-Tsann
authors.initials: MT
authors.lastname: Lai
authors.forename: Fuyong
authors.initials: F
authors.lastname: Du
authors.forename: Amy
authors.initials: A
authors.lastname: Musto
authors.forename: George
authors.initials: G
authors.lastname: Allan
authors.forename: DoWon
authors.initials: D
authors.lastname: Hahn
authors.forename: Scott
authors.initials: S
authors.lastname: Lundeen
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000818:Animals; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001826:Body Fluids / Q000187:drug effects*; D015519:Bone Density / Q000187:drug effects; D002460:Cell Line; D002784:Cholesterol / Q000097:blood; D005260:Female; D019584:Hot Flashes / Q000188:drug therapy*; D006801:Humans; D009929:Organ Size / Q000187:drug effects; D010052:Ovariectomy; D051381:Rats; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D014599:Uterus / Q000187:drug effects; D014621:Vagina / Q000187:drug effects* / Q000378:metabolism; D014623:Vaginal Diseases / Q000188:drug therapy*
chemical_list: D001578:Benzopyrans; D020845:Selective Estrogen Receptor Modulators; D002784:Cholesterol