title: Synthesis and biological properties of novel glucocorticoid androstene C-17 furoate esters.
abstract: A series of novel corticosteroid derivatives featuring C-17 furoate ester functionality have been synthesised. Profiling in vitro and in vivo has resulted in the identification of a compound with a longer duration of action and a lower oral side effect profile in rodents compared to budesonide.
authors.affiliation: Novartis Institutes for Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex, RH12 5AB, United Kingdom. david.sandham@pharma.novartis.com <david.sandham@pharma.novartis.com>
authors.forename: David A
authors.initials: DA
authors.lastname: Sandham
authors.forename: Lucy
authors.initials: L
authors.lastname: Barker
authors.forename: David
authors.initials: D
authors.lastname: Beattie
authors.forename: David
authors.initials: D
authors.lastname: Beer
authors.forename: Louise
authors.initials: L
authors.lastname: Bidlake
authors.forename: David
authors.initials: D
authors.lastname: Bentley
authors.forename: Keith D
authors.initials: KD
authors.lastname: Butler
authors.forename: Sarah
authors.initials: S
authors.lastname: Craig
authors.forename: David
authors.initials: D
authors.lastname: Farr
authors.forename: Claire
authors.initials: C
authors.lastname: Ffoulkes-Jones
authors.forename: John R
authors.initials: JR
authors.lastname: Fozard
authors.forename: Sandra
authors.initials: S
authors.lastname: Haberthuer
authors.forename: Colin
authors.initials: C
authors.lastname: Howes
authors.forename: Deborah
authors.initials: D
authors.lastname: Hynx
authors.forename: Sarah
authors.initials: S
authors.lastname: Jeffers
authors.forename: Thomas H
authors.initials: TH
authors.lastname: Keller
authors.forename: Paul A
authors.initials: PA
authors.lastname: Kirkham
authors.forename: Janet C
authors.initials: JC
authors.lastname: Maas
authors.forename: Lazzaro
authors.initials: L
authors.lastname: Mazzoni
authors.forename: Andrew
authors.initials: A
authors.lastname: Nicholls
authors.forename: Gaynor E
authors.initials: GE
authors.lastname: Pilgrim
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Schaebulin
authors.forename: Gillian M
authors.initials: GM
authors.lastname: Spooner
authors.forename: Rowan
authors.initials: R
authors.lastname: Stringer
authors.forename: Pamela
authors.initials: P
authors.lastname: Tranter
authors.forename: Katharine L
authors.initials: KL
authors.lastname: Turner
authors.forename: Morris F
authors.initials: MF
authors.lastname: Tweed
authors.forename: Christoph
authors.initials: C
authors.lastname: Walker
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Watson
authors.forename: Bernard M
authors.initials: BM
authors.lastname: Cuenoud
mesh_terms: D000736:Androstenes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001682:Biological Availability; D002460:Cell Line; D004802:Eosinophilia / Q000188:drug therapy; D004952:Esters / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D005938:Glucocorticoids / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D008264:Macrophages / Q000166:cytology; D009929:Organ Size / Q000187:drug effects; D011485:Protein Binding; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000819:agonists*; D013329:Structure-Activity Relationship; D013950:Thymus Gland / Q000187:drug effects; D014409:Tumor Necrosis Factor-alpha / Q000032:analysis / Q000037:antagonists & inhibitors
chemical_list: D000736:Androstenes; D004952:Esters; D005938:Glucocorticoids; D011965:Receptors, Glucocorticoid; D014409:Tumor Necrosis Factor-alpha