3,5-Bis(trifluoromethyl)pyrazoles: A Novel Class of NFAT Transcription Factor Regulator
Journal of Medicinal Chemistry2000Vol. 43(16), pp. 2975–2981
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Stevan W. Djurić, Nwe Y. BaMaung, Anwer Basha, Huaqing Liu, Jay R. Luly, David J. Madar, Richard J. Sciotti, Noah P. Tu, Frank L. Wagenaar, Paul E. Wiedeman, Xun Zhou, Stephen J. Ballaron, Joy Bauch, Yung‐Wu Chen, X. Grace Chiou, Thomas A. Fey, Donna M. Gauvin, Earl J. Gubbins, Gin C. Hsieh, Kennan C. Marsh, Karl W. Mollison, Melissa Pong, Thomas K. Shaughnessy, Michael P. Sheets, Morey L. Smith, James M. Trevillyan, Usha Warrior, Craig D. Wegner, George W. Carter
Abstract
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 not directly inhibit the dephosphorylation of NFAT by calcineurin.
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