The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

Simple 1-substituted 5- and 6-isoxazolyl-benzimidazoles have been shown to be potent inhibitors of the BET bromodomains with selectivity over the related bromodomain of CBP. The reported inhibitors were prepared from simple starting materials in two steps followed by separation of the regioisomers o...

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Veröffentlicht in:Medchemcomm
Hauptverfasser: Hay, Duncan, Fedorov, Oleg, Filippakopoulos, Panagis, Martin, Sarah, Philpott, Martin, Picaud, Sarah, Hewings, David S., Uttakar, Sagar, Heightman, Tom D., Conway, Stuart J., Knapp, Stefan, Brennan, Paul E.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2013
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4678575/
https://ncbi.nlm.nih.gov/pubmed/26682033
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/C2MD20189E
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