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New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

[Image: see text] We describe new synthetic routes developed toward a range of substituted analogues of bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo-benzodiazepine scaffold. These new routes allow for the derivatization of the methoxyphenyl and chloropheny...

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Detalles Bibliográficos
Autores principales: Baud, Matthias G. J., Lin-Shiao, Enrique, Zengerle, Michael, Tallant, Cynthia, Ciulli, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2015
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4770307/
https://www.ncbi.nlm.nih.gov/pubmed/26367539
http://dx.doi.org/10.1021/acs.jmedchem.5b01135