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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Hauptverfasser: 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.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2013
Online Zugang: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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