Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives

Bioorg Med Chem Lett. 2000 Apr 3;10(7):619-22. doi: 10.1016/s0960-894x(00)00066-4.


We have designed and synthesized a series of pyrazole derivatives as candidate retinoic acid receptor (RAR) agonists. One of them, 4-[5-(1, 5-diisopropyl-1H-3-pyrazolyl)-1H-2-pyrrolyl]benzoic acid (11b), which possesses a 2,5-disubstituted pyrrole moiety, showed selective transactivation activity for the RAR alpha receptor, and had highly potent cell-differentiating activity on HL-60 cells.

MeSH terms

  • Binding, Competitive
  • Cell Differentiation / drug effects
  • HL-60 Cells
  • Humans
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology
  • Receptors, Retinoic Acid / agonists*
  • Retinoic Acid Receptor alpha
  • Structure-Activity Relationship


  • Pyrazoles
  • RARA protein, human
  • Receptors, Retinoic Acid
  • Retinoic Acid Receptor alpha