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

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

Author information

1
Department of Chemistry, University of Illinois, Urbana, IL 61801, USA.

Abstract

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.

PMID:
19014882
PMCID:
PMC2711511
DOI:
10.1016/j.bmcl.2008.11.006
[Indexed for MEDLINE]
Free PMC Article

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