title: Discovery of a new class of p38 kinase inhibitors.
abstract: The MAP kinase p38 has been implicated in cytokine signaling, and its inhibitors are potentially useful for the treatment of arthritis and osteoporosis. Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and exhibit activity in the nanomolar range. Very steep structure-activity relationships are observed within this class.
authors.affiliation: Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA. jacques.dumas.b@bayer.com
authors.forename: J
authors.initials: J
authors.lastname: Dumas
authors.forename: R
authors.initials: R
authors.lastname: Sibley
authors.forename: B
authors.initials: B
authors.lastname: Riedl
authors.forename: M K
authors.initials: MK
authors.lastname: Monahan
authors.forename: W
authors.initials: W
authors.lastname: Lee
authors.forename: T B
authors.initials: TB
authors.lastname: Lowinger
authors.forename: A M
authors.initials: AM
authors.lastname: Redman
authors.forename: J S
authors.initials: JS
authors.lastname: Johnson
authors.forename: J
authors.initials: J
authors.lastname: Kingery-Wood
authors.forename: W J
authors.initials: WJ
authors.lastname: Scott
authors.forename: R A
authors.initials: RA
authors.lastname: Smith
authors.forename: M
authors.initials: M
authors.lastname: Bobko
authors.forename: R
authors.initials: R
authors.lastname: Schoenleber
authors.forename: G E
authors.initials: GE
authors.lastname: Ranges
authors.forename: T J
authors.initials: TJ
authors.lastname: Housley
authors.forename: A
authors.initials: A
authors.lastname: Bhargava
authors.forename: S M
authors.initials: SM
authors.lastname: Wilhelm
authors.forename: A
authors.initials: A
authors.lastname: Shrikhande
mesh_terms: D018501:Antirheumatic Agents / Q000138:chemical synthesis / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000737:chemistry; D006801:Humans; D006843:Hydrocarbons, Chlorinated / Q000737:chemistry; D020128:Inhibitory Concentration 50; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D010024:Osteoporosis / Q000188:drug therapy; D010671:Phenylurea Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases
chemical_list: D018501:Antirheumatic Agents; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D006843:Hydrocarbons, Chlorinated; D010671:Phenylurea Compounds; D020928:Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases