Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927

[Image: see text] The further optimization of ER-α degradation efficacy of a series of ER modulators by refining side-chain substitution led to efficacious selective estrogen receptor degraders (SERDs). A fluoromethyl azetidine group was found to be preferred and resulted in the identification of bi...

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Udgivet i:ACS Med Chem Lett
Main Authors: Kahraman, Mehmet, Govek, Steven P., Nagasawa, Johnny Y., Lai, Andiliy, Bonnefous, Celine, Douglas, Karensa, Sensintaffar, John, Liu, Nhin, Lee, KyoungJin, Aparicio, Anna, Kaufman, Josh, Qian, Jing, Shao, Gang, Prudente, Rene, Joseph, James D., Darimont, Beatrice, Brigham, Daniel, Heyman, Richard, Rix, Peter J., Hager, Jeffrey H., Smith, Nicholas D.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2018
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6331158/
https://ncbi.nlm.nih.gov/pubmed/30655946
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00414
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