1129606-89-8Relevant articles and documents
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity
Yu, Wensheng,Liu, Jian,Clausen, Dane,Yu, Younong,Duffy, Joseph L.,Wang, Ming,Xu, Shouning,Deng, Lin,Suzuki, Takao,Chung, Christine C.,Myers, Robert W.,Klein, Daniel J.,Fells, James I.,Holloway, M. Katharine,Wu, Jin,Wu, Guoxin,Howell, Bonnie J.,Barnard, Richard J. O.,Kozlowski, Joseph
supporting information, p. 4709 - 4729 (2021/05/07)
We describe the discovery of histone deacetylase (HDACs) 1, 2, and 3 inhibitors with ethyl ketone as the zinc-binding group. These HDACs 1, 2, and 3 inhibitors have good enzymatic and cellular activity. Their serum shift in cellular potency has been minimized, and selectivity against hERG has been improved. They are also highly selective over HDACs 6 and 8. These inhibitors contain a variety of substituted heterocycles on the imidazole or oxazole scaffold. Compounds 31 and 48 stand out due to their good potency, high selectivity over HDACs 6 and 8, reduced hERG activity, optimized serum shift in cellular potency, and good rat and dog PK profiles.
Tandem copper-catalysed aryl and alkenyl amination reactions: The synthesis of N-functionalised indoles
Hodgkinson, Roy C.,Schulz, Jurgen,Willis, Michael C.
supporting information; experimental part, p. 432 - 434 (2009/06/28)
A Cu-diamine complex effectively catalyses tandem C-N bond formation on 2-(2-haloalkenyl)-aryl halide substrates, to deliver a series of N-functionalised indoles. Anilines, amides and carbamates are all effective coupling partners under the developed cond
