title: Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
abstract: A series of purine based inhibitors of PDE7 has been derived from screening lead 1a. The synthesis, structure-activity relationships (SAR), and selectivity against several other PDE family members are described.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. pittsw@bms.com
authors.forename: William J
authors.initials: WJ
authors.lastname: Pitts
authors.forename: Wayne
authors.initials: W
authors.lastname: Vaccaro
authors.forename: Tram
authors.initials: T
authors.lastname: Huynh
authors.forename: Katerina
authors.initials: K
authors.lastname: Leftheris
authors.forename: Jacques Y
authors.initials: JY
authors.lastname: Roberge
authors.forename: Joseph
authors.initials: J
authors.lastname: Barbosa
authors.forename: Junqing
authors.initials: J
authors.lastname: Guo
authors.forename: Baerbel
authors.initials: B
authors.lastname: Brown
authors.forename: Andrew
authors.initials: A
authors.lastname: Watson
authors.forename: Karen
authors.initials: K
authors.lastname: Donaldson
authors.forename: Gary C
authors.initials: GC
authors.lastname: Starling
authors.forename: Peter A
authors.initials: PA
authors.lastname: Kiener
authors.forename: Michael A
authors.initials: MA
authors.lastname: Poss
authors.forename: John H
authors.initials: JH
authors.lastname: Dodd
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D001665:Binding Sites; D002460:Cell Line; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000201:enzymology
chemical_list: D004791:Enzyme Inhibitors; D008024:Ligands; D011687:Purines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7