Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

[Image: see text] The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-based drug design effort lead to a novel isoxazole azepine scaffold. This scaffold showed go...

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Autori principali: Gehling, Victor S., Hewitt, Michael C., Vaswani, Rishi G., Leblanc, Yves, Côté, Alexandre, Nasveschuk, Christopher G., Taylor, Alexander M., Harmange, Jean-Christophe, Audia, James E., Pardo, Eneida, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A., Sims, Robert J., Bergeron, Louise, Bryant, Barbara M., Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Sankaranarayanan, Ravichandran, Yellapantula, Sreegouri, Bangalore Srinivasamurthy, Nandana, Birudukota, Swarnakumari, Albrecht, Brian K.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2013
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027525/
https://ncbi.nlm.nih.gov/pubmed/24900758
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml4001485
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