Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase.
The p38 MAP kinase is implicated in the release of the pro-inflammatory cytokines TNFalpha and IL-1b. Inhibition of cytokine release may be a useful treatment for inflammatory conditions such as rheumatoid arthritis and Crohn's disease. A new lead structure for p38 MAP kinase inhibition was identified. Herein, we report the SAR of this new class of p38 inhibitors.
Laufer
Stefan
S
Institute of Pharmacy, Department of Pharmaceutical and Medicinal Chemistry, Eberhard-Karls-University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
Lehmann
Frank
F
D001665:Binding Sites / Q000502:physiology; D018360:Crystallography, X-Ray; D055808:Drug Discovery; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
D007211:Indoles; D047428:Protein Kinase Inhibitors; C499748:SCIO-469; D048051:p38 Mitogen-Activated Protein Kinases