title: Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation.
abstract: A series of pyrimidine based inhibitors of PDE7 are discussed. The synthesis, structure-activity relationships (SAR) and selectivity against several other PDE family members as well as activity in T cells are presented. These compounds were found to have effects on T cell proliferation, however it is not clear whether the mechanism is related to PDE7 inhibition.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. junqing.guo@bms.com
authors.forename: Junqing
authors.initials: J
authors.lastname: Guo
authors.forename: Andrew
authors.initials: A
authors.lastname: Watson
authors.forename: James
authors.initials: J
authors.lastname: Kempson
authors.forename: Marianne
authors.initials: M
authors.lastname: Carlsen
authors.forename: Joseph
authors.initials: J
authors.lastname: Barbosa
authors.forename: Karen
authors.initials: K
authors.lastname: Stebbins
authors.forename: Deborah
authors.initials: D
authors.lastname: Lee
authors.forename: John
authors.initials: J
authors.lastname: Dodd
authors.forename: Steven G
authors.initials: SG
authors.lastname: Nadler
authors.forename: Murray
authors.initials: M
authors.lastname: McKinnon
authors.forename: Joel
authors.initials: J
authors.lastname: Barrish
authors.forename: William J
authors.initials: WJ
authors.lastname: Pitts
mesh_terms: D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D055786:Gene Knockout Techniques; D051379:Mice; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects* / Q000276:immunology
chemical_list: D010726:Phosphodiesterase Inhibitors; D011743:Pyrimidines; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7