Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat

[Image: see text] A series of tetrahydroisoquinoline phenols was modified to give an estrogen receptor downregulator-antagonist profile. Optimization around the core, alkyl side chain, and pendant aryl ring resulted in compounds with subnanomolar levels of potency. The phenol functionality was shown...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: Scott, James S., Bailey, Andrew, Davies, Robert D. M., Degorce, Sébastien L., MacFaul, Philip A., Gingell, Helen, Moss, Thomas, Norman, Richard A., Pink, Jennifer H., Rabow, Alfred A., Roberts, Bryan, Smith, Peter D.
Format: Artigo
Language:Inglês
Published: American Chemical Society 2015
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4716595/
https://ncbi.nlm.nih.gov/pubmed/26819673
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00413
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