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

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. This journal is © The Royal Society of Chemistry 2013.
Publication status:
Published

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Publisher copy:
10.1039/c2md20189e

Authors


Fedorov, O More by this author
More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Philpott, M More by this author
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Journal:
MEDCHEMCOMM
Volume:
4
Issue:
1
Pages:
140-144
Publication date:
2013-01-05
DOI:
EISSN:
2040-2511
ISSN:
2040-2503
URN:
uuid:7affc0c5-1100-4f51-9288-143ff874bfa8
Source identifiers:
375356
Local pid:
pubs:375356
Language:
English

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