title: Synthesis of 2alpha-substituted-14-epi-previtamin D3 and its genomic activity.
abstract: We synthesized and isolated 2 alpha-substituted analogs of 14-epi-previtamin D3 after thermal isomerization at 80 degrees C for the first time. The VDR binding affinity and transactivation activity of osteocalcin promoter in HOS cells were evaluated, and the 2 alpha-methyl-substituted analog was found to have greater genomic activity than 14-epi-previtamin D3.
authors.affiliation: Faculty of Pharmaceutical Sciences, Teikyo University, Sagamiko, Kanagawa 229-0195, Japan.
authors.forename: Daisuke
authors.initials: D
authors.lastname: Sawada
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Katayama
authors.forename: Yuya
authors.initials: Y
authors.lastname: Tsukuda
authors.forename: Nozomi
authors.initials: N
authors.lastname: Saito
authors.forename: Masashi
authors.initials: M
authors.lastname: Takano
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Saito
authors.forename: Ken-Ichiro
authors.initials: K
authors.lastname: Takagi
authors.forename: Eiji
authors.initials: E
authors.lastname: Ochiai
authors.forename: Seiichi
authors.initials: S
authors.lastname: Ishizuka
authors.forename: Kazuya
authors.initials: K
authors.lastname: Takenouchi
authors.forename: Atsushi
authors.initials: A
authors.lastname: Kittaka
mesh_terms: D045744:Cell Line, Tumor; D002762:Cholecalciferol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015675:Osteocalcin / Q000235:genetics*; D011401:Promoter Regions, Genetic / Q000187:drug effects*; D011485:Protein Binding; D018167:Receptors, Calcitriol / Q000378:metabolism*; D014815:Vitamins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D018167:Receptors, Calcitriol; D014815:Vitamins; D015675:Osteocalcin; D002762:Cholecalciferol; C025168:previtamin D(3)