Design and Optimization of Benzopiperazines as Potent Inhibitors of BET Bromodomains

[Image: see text] A protein structure-guided drug design approach was employed to develop small molecule inhibitors of the BET family of bromodomains that were distinct from the known (+)-JQ1 scaffold class. These efforts led to the identification of a series of substituted benzopiperazines with str...

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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: Millan, David S., Kayser-Bricker, Katherine J., Martin, Matthew W., Talbot, Adam C., Schiller, Shawn E. R., Herbertz, Torsten, Williams, Grace L., Luke, George P., Hubbs, Stephen, Alvarez Morales, Monica A., Cardillo, Daniel, Troccolo, Paul, Mendes, Rachel L., McKinnon, Crystal
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2017
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5554895/
https://ncbi.nlm.nih.gov/pubmed/28835800
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00191
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