title: Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.
abstract: A novel series of 17beta-hydroxysteroid dehydrogenase type 3 (17beta-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17beta-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays.
authors.affiliation: Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. brian.fink@bms.com
authors.forename: Brian E
authors.initials: BE
authors.lastname: Fink
authors.forename: Ashvinikumar V
authors.initials: AV
authors.lastname: Gavai
authors.forename: John S
authors.initials: JS
authors.lastname: Tokarski
authors.forename: Bindu
authors.initials: B
authors.lastname: Goyal
authors.forename: Raj
authors.initials: R
authors.lastname: Misra
authors.forename: Hai-Yun
authors.initials: HY
authors.lastname: Xiao
authors.forename: S David
authors.initials: SD
authors.lastname: Kimball
authors.forename: Wen-Ching
authors.initials: WC
authors.lastname: Han
authors.forename: Derek
authors.initials: D
authors.lastname: Norris
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Spires
authors.forename: Dan
authors.initials: D
authors.lastname: You
authors.forename: Marco M
authors.initials: MM
authors.lastname: Gottardis
authors.forename: Matthew V
authors.initials: MV
authors.lastname: Lorenzi
authors.forename: Gregory D
authors.initials: GD
authors.lastname: Vite
mesh_terms: D015067:17-Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000469:Alkaline Phosphatase / Q000187:drug effects / Q000378:metabolism; D000735:Androstenedione / Q000378:metabolism; D001392:Azocines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013739:Testosterone / Q000096:biosynthesis
chemical_list: D001392:Azocines; D004791:Enzyme Inhibitors; D013739:Testosterone; D000735:Androstenedione; D015067:17-Hydroxysteroid Dehydrogenases; C476565:17beta-hydroxysteroid dehydrogenase type 3; D000469:Alkaline Phosphatase