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Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide
1i (4-[5-(4-methylphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis, is identified. Expand
A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts.
The effect of SC-514 on cytokine gene expression may be a combination of inhibiting I kappa B alphaosphorylation/degradation, affecting NF-kappa B nuclear import/export as well as the phosphorylation and transactivation of p65. Expand
A Selective IKK-2 Inhibitor Blocks NF-κB-dependent Gene Expression in Interleukin-1β-stimulated Synovial Fibroblasts*
The effect of SC-514 on cytokine gene expression may be a combination of inhibiting IκBα phosphorylation/degradation, affecting NF-κB nuclear import/export as well as the phosphorylated and transactivation of p65. Expand
The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: the second clinical candidate having a shorter and favorable human half-life.
In this Letter, we provide the structure-activity relationships, optimization of design, testing criteria, and human half-life data for a series of selective COX-2 inhibitors. During the course ofExpand
Pharmacology of PF-4191834, a Novel, Selective Non-Redox 5-Lipoxygenase Inhibitor Effective in Inflammation and Pain
The combination of potency in cells and in vivo, together with a sustained in vivo effect, provides PF-4191834 with an overall pharmacodynamic improvement consistent with once a day dosing. Expand
Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.
In the synthesis of selective COX-2 inhibitors, the sulfonamide moiety is a suitable replacement for the methylsulfonyl moiety yielding compounds with activity both in vitro and in vivo. Expand
Synthesis, crystal structure, and activity of pyrazole-based inhibitors of p38 kinase.
A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of 1 (SC-102) bound to p38 enzyme, and a compound identified from this series was efficacious in an animal model of rheumatic disease. Expand
CJ-13610, an orally active inhibitor of 5-lipoxygenase is efficacious in preclinical models of pain.
The data suggest that 5-LOX pathway and the leukotriene products are important mediators of pain. Expand
The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.
The discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors is reported. Expand