Analogs of methyl-piperidinopyrazole (MPP): Antiestrogens with estrogen receptor α selective activity

Hai Bing Zhou, Kathryn E. Carlson, Fabio Stossi, Benita S Katzenellenbogen, John A. Katzenellenbogen

Research output: Contribution to journalArticle

Abstract

Methyl-piperidino-pyrazole (MPP), an estrogen receptor α (ERα)-selective antagonist we developed, has a basic side chain (BSC) attached to an ERα-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 ERα-selective binding affinity and antagonist potency of MPP.

Original languageEnglish (US)
Pages (from-to)108-110
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number1
DOIs
StatePublished - Jan 1 2009

Fingerprint

Estrogen Receptor Modulators
Estrogen Receptors
Ether
Estrogens
Ligands
pyrazole

Keywords

  • Antiestrogen
  • Estrogen receptor antagonist
  • PPT
  • Propyl piperidino triol
  • Subtype-selective ligand

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Analogs of methyl-piperidinopyrazole (MPP) : Antiestrogens with estrogen receptor α selective activity. / Zhou, Hai Bing; Carlson, Kathryn E.; Stossi, Fabio; Katzenellenbogen, Benita S; Katzenellenbogen, John A.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 1, 01.01.2009, p. 108-110.

Research output: Contribution to journalArticle

Zhou, Hai Bing ; Carlson, Kathryn E. ; Stossi, Fabio ; Katzenellenbogen, Benita S ; Katzenellenbogen, John A. / Analogs of methyl-piperidinopyrazole (MPP) : Antiestrogens with estrogen receptor α selective activity. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 1. pp. 108-110.
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