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Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry

[Image: see text] Herein we report the use of metathesis to construct a novel tetracyclic core in a series of estrogen receptor degraders. This improved the chemical stability, as assessed using an NMR-MS based assay, and gave a molecule with excellent physicochemical properties and pharmacokinetics...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Scott, James S., Breed, Jason, Carbajo, Rodrigo J., Davey, Paul R., Greenwood, Ryan, Huynh, Hoan K., Klinowska, Teresa, Morrow, Christopher J., Moss, Thomas A., Polanski, Radoslaw, Nissink, J. Willem M., Varnes, Jeffrey, Yang, Bin
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6792171/
https://ncbi.nlm.nih.gov/pubmed/31620239
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00370
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