Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 1, Pages 108-110Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.006
Keywords
Estrogen receptor antagonist; Antiestrogen; Subtype-selective ligand; PPT; Propyl piperidino triol
Categories
Funding
- NIH [PHS 5R37 DK15556, 5R01 CA11819]
- Keck Foundation
- NIH
- NSF
- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [R37DK015556] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE ON DEAFNESS AND OTHER COMMUNICATION DISORDERS [R01DC011819] Funding Source: NIH RePORTER
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
