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

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

  • J Med Chem. 2000 Aug 10;43(16):2975-81. doi: 10.1021/jm990615a.
S W Djuric 1,  N Y BaMaung,  A Basha,  H Liu,  J R Luly,  D J Madar,  R J Sciotti,  N P Tu,  F L Wagenaar,  P E Wiedeman,  X Zhou,  S Ballaron,  J Bauch,  Y W Chen,  X G Chiou,  T Fey,  D Gauvin,  E Gubbins,  G C Hsieh,  K C Marsh,  K W Mollison,  M Pong,  T K Shaughnessy,  M P Sheets,  M Smith,  J M Trevillyan,  U Warrior,  C D Wegner,  G W Carter
Affiliations

Affiliation

  • 1 Immunological Diseases Research, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, Illinois 60064-6217, USA. stevan.w.djuric@abbott.com
PMID: 10956206 DOI: 10.1021/jm990615a
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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