BET Bromodomain Inhibitors With One-step Synthesis Discovered from Virtual Screen

Chemical inhibition of epigenetic regulatory proteins BrdT and Brd4 is emerging as a promising therapeutic strategy in contraception, cancer, and heart disease. We report an easily synthesized dihydropyridopyrimidine pan-BET inhibitor scaffold, which was uncovered via a virtual screen followed by te...

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Publicado en:J Med Chem
Main Authors: Ayoub, Alex M., Hawk, Laura M. L., Herzig, Ryan J., Jiang, Jiewei, Wisniewski, Andrea J., Gee, Clifford T., Zhao, Peiliang, Zhu, Jin-Yi, Berndt, Norbert, Offei-Addo, Nana K., Scott, Thomas G., Qi, Jun, Bradner, James E., Ward, Timothy R., Schönbrunn, Ernst, Georg, Gunda I., Pomerantz, William C.K.
Formato: Artigo
Idioma:Inglês
Publicado: 2017
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC5558211/
https://ncbi.nlm.nih.gov/pubmed/28535045
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01336
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