The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
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DOI：
10.1039/c2md20189e
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发表时间：
2013-01-01
期刊：
影响因子：
--
通讯作者：
Brennan PE
中科院分区：
文献类型：
--
作者：
Hay D;Fedorov O;Filippakopoulos P;Martin S;Philpott M;Picaud S;Hewings DS;Uttakar S;Heightman TD;Conway SJ;Knapp S;Brennan PE
简单的1-取代的5-和6-异恶唑基-苯并咪唑已被证明是BET溴结构域的有效抑制剂，其选择性超过CBP的相关溴结构域。所报道的抑制剂是从简单的起始原料分两步制备的，然后分三步分离区域异构体或区域选择性地分离。
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.