title: Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.
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.
authors.affiliation: Department of Chemistry, University of Illinois, Urbana, IL 61801, USA.
authors.forename: Hai-Bing
authors.initials: HB
authors.lastname: Zhou
authors.forename: Kathryn E
authors.initials: KE
authors.lastname: Carlson
authors.forename: Fabio
authors.initials: F
authors.lastname: Stossi
authors.forename: Benita S
authors.initials: BS
authors.lastname: Katzenellenbogen
authors.forename: John A
authors.initials: JA
authors.lastname: Katzenellenbogen
mesh_terms: D020847:Estrogen Receptor Modulators / Q000138:chemical synthesis*; D047628:Estrogen Receptor alpha / Q000187:drug effects*; D006801:Humans; D008024:Ligands; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D020847:Estrogen Receptor Modulators; D047628:Estrogen Receptor alpha; D008024:Ligands; D010880:Piperidines; D011720:Pyrazoles