The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains. Hay, D., Fedorov, O., Filippakopoulos, P., Martin, S., Philpott, M., Picaud, S., Hewings, D., S., Uttakar, S., Heightman, T., D., Conway, S., J., Knapp, S., & Brennan, P., E. MedChemComm, 4(1):140-144, The Royal Society of Chemistry, 2013.
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains [pdf]Paper  The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains [link]Website  doi  abstract   bibtex   
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

Downloads: 0