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Issue 1, 2013
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The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

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Abstract

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 or regioselectively in three steps.

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

  • This article is part of the themed collection: New Talent
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Publication details

The article was received on 29 May 2012, accepted on 10 Aug 2012 and first published on 13 Aug 2012


Article type: Concise Article
DOI: 10.1039/C2MD20189E
Med. Chem. Commun., 2013,4, 140-144

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

    D. Hay, O. Fedorov, P. Filippakopoulos, S. Martin, M. Philpott, S. Picaud, D. S. Hewings, S. Uttakar, T. D. Heightman, S. J. Conway, S. Knapp and P. E. Brennan, Med. Chem. Commun., 2013, 4, 140
    DOI: 10.1039/C2MD20189E

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