The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains
MedChemComm2012Vol. 4(1), pp. 140–144
Citations Over TimeTop 10% of 2012 papers
Duncan A. Hay, O. Fedorov, P. Filippakopoulos, Sarah Martin, Martin Philpott, S. Picaud, David S. Hewings, Sagar Uttakar, Tom D. Heightman, Stuart J. Conway, Stefan Knapp, Paul E. Brennan
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.
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