Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity

Bioorg Med Chem Lett. 2009 Jan 1;19(1):108-10. doi: 10.1016/j.bmcl.2008.11.006. Epub 2008 Nov 6.


Methyl-piperidino-pyrazole (MPP), an estrogen receptor alpha (ERalpha)-selective antagonist we developed, has a basic side chain (BSC) attached to an ERalpha-selective agonist ligand, methyl-pyrazole-triol (MPT) through an ether linkage. To remove the possibility that metabolic cleavage of the BSC in MPP would regenerate MPT, we have replaced the N-piperidinylethoxy moiety with an N-piperidinylpropyl group, giving MPrP. This new analog retains the high ERalpha-selective binding affinity and antagonist potency of MPP.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Estrogen Receptor Modulators / chemical synthesis*
  • Estrogen Receptor alpha / drug effects*
  • Humans
  • Ligands
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Structure-Activity Relationship


  • Estrogen Receptor Modulators
  • Estrogen Receptor alpha
  • Ligands
  • Piperidines
  • Pyrazoles