Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.
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.
Zhou
Hai-Bing
HB
Department of Chemistry, University of Illinois, Urbana, IL 61801, USA.
Carlson
Kathryn E
KE
Stossi
Fabio
F
Katzenellenbogen
Benita S
BS
Katzenellenbogen
John A
JA
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
D020847:Estrogen Receptor Modulators; D047628:Estrogen Receptor alpha; D008024:Ligands; D010880:Piperidines; D011720:Pyrazoles