TY - JOUR
T1 - Analogs of methyl-piperidinopyrazole (MPP)
T2 - Antiestrogens with estrogen receptor α selective activity
AU - Zhou, Hai Bing
AU - Carlson, Kathryn E.
AU - Stossi, Fabio
AU - Katzenellenbogen, Benita S.
AU - Katzenellenbogen, John A.
N1 - Funding Information:
Supported by grants from the NIH (PHS 5R37 DK15556 to J.A.K. and 5R01 CA11819 to B.S.K.). Funding for NMR and MS instrumentation is from the Keck Foundation, NIH and NSF. We are grateful to Dr. Sung Hoon Kim and Dr. William A. Boulanger for helpful comments.
PY - 2009/1/1
Y1 - 2009/1/1
N2 - 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.
AB - 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.
KW - Antiestrogen
KW - Estrogen receptor antagonist
KW - PPT
KW - Propyl piperidino triol
KW - Subtype-selective ligand
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U2 - 10.1016/j.bmcl.2008.11.006
DO - 10.1016/j.bmcl.2008.11.006
M3 - Article
C2 - 19014882
AN - SCOPUS:57749097014
SN - 0960-894X
VL - 19
SP - 108
EP - 110
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 1
ER -