| Literature DB >> 32331932 |
Wensheng Yu1, Jian Liu2, Younong Yu2, Vivian Zhang2, Dane Clausen2, Joseph Kelly2, Scott Wolkenberg3, Douglas Beshore3, Joseph L Duffy2, Christine C Chung2, Robert W Myers2, Daniel J Klein3, James Fells3, Kate Holloway3, Jin Wu2, Guoxin Wu3, Bonnie J Howell3, Richard J O Barnard3, Joseph Kozlowski2.
Abstract
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.Entities:
Keywords: 2C4 cells; HDAC inhibitor; HDACs 1, 2, 3; HDACs 6, 8; HIV latency; HIV latency reversing agent; Shock and kill; Zinc binding group
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Year: 2020 PMID： 32331932 DOI： 10.1016/j.bmcl.2020.127197
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823