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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Publicado en:ACS Med Chem Lett
Main Authors: 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
Formato: Artigo
Idioma:Inglês
Publicado: American Chemical Society 2017
Acceso en liña: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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