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Issue 1, 2013

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

Supplementary files

Article information


Submitted
29 May 2012
Accepted
10 Aug 2012
First published
13 Aug 2012

Med. Chem. Commun., 2013,4, 140-144
Article type
Concise Article

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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