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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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Detalhes bibliográficos
Publicado no: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.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha: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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