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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Udgivet i: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
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2019
Online adgang: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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