3, 5-Bis (trifluoromethyl) pyrazoles: a novel class of NFAT transcription factor regulator

…, KW Mollison, M Pong, TK Shaughnessy…

文献索引：Djuric; Wiedeman; Zhou; Ballaron; Bauch; Chen; Chiou; Fey; Gauvin; Gubbins; Hsieh; Bamaung; Marsh; Mollison; Pong; Shaughnessy; Sheets; Smith; Trevillyan; Warrior; Wegner; Carter; Basha; Liu; Luly; Madar; Sciotti; Tu; Wagenaar Journal of Medicinal Chemistry, 2000 , vol. 43, # 16 p. 2975 - 2981

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被引用次数: 114

摘要

A series of bis (trifluoromethyl) pyrazoles (BTPs) has been found to be a novel inhibitor of cytokine production. Identified initially as inhibitors of IL-2 synthesis, the BTPs have been optimized in this regard and even inhibit IL-2 production with a 10-fold enhancement over cyclosporine in an ex vivo assay. Additionally, the BTPs show inhibition of IL-4, IL-5, IL-8, and eotaxin production. Unlike the IL-2 inhibitors, cyclosporine and FK506, the BTPs do ...