title: Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.
abstract: The synthesis, physicochemical properties and pharmacological profiles of two novel silicon-containing p38 MAP kinase inhibitors are described.
authors.affiliation: Paradigm Therapeutics Ltd, 418 Cambridge Science Park, Milton Road, Cambridge CB4 0PA, UK.
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Barnes
authors.forename: Richard
authors.initials: R
authors.lastname: Conroy
authors.forename: David J
authors.initials: DJ
authors.lastname: Miller
authors.forename: John S
authors.initials: JS
authors.lastname: Mills
authors.forename: John G
authors.initials: JG
authors.lastname: Montana
authors.forename: Parminder K
authors.initials: PK
authors.lastname: Pooni
authors.forename: Graham A
authors.initials: GA
authors.lastname: Showell
authors.forename: Louise M
authors.initials: LM
authors.lastname: Walsh
authors.forename: Julie B H
authors.initials: JB
authors.lastname: Warneck
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D008862:Microsomes, Liver / Q000201:enzymology / Q000378:metabolism; D008958:Models, Molecular; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D017655:Silicon Compounds / Q000737:chemistry*; D013237:Stereoisomerism; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D008070:Lipopolysaccharides; D011720:Pyrazoles; D017655:Silicon Compounds; D014409:Tumor Necrosis Factor-alpha; D048051:p38 Mitogen-Activated Protein Kinases