化学
酮
效力
选择性
酰胺
酶
立体化学
化学合成
组合化学
生物化学
有机化学
体外
催化作用
作者
Wei Yu,Jian Liu,Younong Yu,Vivian Zhang,Dane J. Clausen,Joseph M. Kelly,S. E. Wolkenberg,Douglas C. Beshore,Joseph Duffy,Caroline Chung,Robert W. Myers,Daniel Klein,James I. Fells,Kate Holloway,Wei Jin,Guoxin Wu,Bonnie J. Howell,Richard Barnard,Joseph A. Kozlowski
标识
DOI:10.1016/j.bmcl.2020.127197
摘要
A novel series of ethyl ketone based HDACs 1, 2, and 3 selective inhibitors have been identified with good enzymatic and cellular activity and high selectivity over HDACs 6 and 8. These inhibitors contain a spirobicyclic group in the amide region. Compound 13 stands out as a lead due to its good potency, high selectivity, and reasonable rat and dog PK. Compounds 33 and 34 show good potency and rat PK profiles as well.
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