title: Potent, low-calcemic, selective inhibitors of CYP24 hydroxylase: 24-sulfone analogs of the hormone 1alpha,25-dihydroxyvitamin D3.
abstract: The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1alpha,25-dihydroxyvitamin D(3), is a potent (IC(50) = 28nM) and highly selective inhibitor of the human 24-hydroxylase enzyme CYP24.
authors.affiliation: Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N. Charles Street, Baltimore, MD 21218-2685, USA. ghp@jhu.edu
authors.forename: Gary H
authors.initials: GH
authors.lastname: Posner
authors.forename: Kenneth R
authors.initials: KR
authors.lastname: Crawford
authors.forename: Hong Woon
authors.initials: HW
authors.lastname: Yang
authors.forename: Mehmet
authors.initials: M
authors.lastname: Kahraman
authors.forename: Heung Bae
authors.initials: HB
authors.lastname: Jeon
authors.forename: Hongbin
authors.initials: H
authors.lastname: Li
authors.forename: Jae Kyoo
authors.initials: JK
authors.lastname: Lee
authors.forename: Byung Chul
authors.initials: BC
authors.lastname: Suh
authors.forename: Mark A
authors.initials: MA
authors.lastname: Hatcher
authors.forename: Tanzina
authors.initials: T
authors.lastname: Labonte
authors.forename: Aimee
authors.initials: A
authors.lastname: Usera
authors.forename: Patrick M
authors.initials: PM
authors.lastname: Dolan
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Kensler
authors.forename: Sara
authors.initials: S
authors.lastname: Peleg
authors.forename: Glenville
authors.initials: G
authors.lastname: Jones
authors.forename: Anqi
authors.initials: A
authors.lastname: Zhang
authors.forename: Bozena
authors.initials: B
authors.lastname: Korczak
authors.forename: Uttam
authors.initials: U
authors.lastname: Saha
authors.forename: Samuel S
authors.initials: SS
authors.lastname: Chuang
mesh_terms: D000818:Animals; D002117:Calcitriol / Q000031:analogs & derivatives / Q000494:pharmacology*; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D013057:Spectrum Analysis; D013250:Steroid Hydroxylases / Q000037:antagonists & inhibitors*; D013450:Sulfones / Q000737:chemistry*; D014158:Transcription, Genetic / Q000187:drug effects; D065668:Vitamin D3 24-Hydroxylase
chemical_list: D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D013450:Sulfones; D013250:Steroid Hydroxylases; D065668:Vitamin D3 24-Hydroxylase; D002117:Calcitriol