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

Methyl-piperidino-pyrazole (MPP), an estrogen receptor alpha (ER alpha)-selective antagonist we developed, has a basic side chain (BSC) attached to an ER alpha-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 ERa-selective binding affinity and antagonist potency of MPP. (C) 2008 Elsevier Ltd. All rights reserved.