Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Wensheng Yu,Jian Liu,Younong Yu,Vivian Zhang,Dane Clausen,Joseph Kelly, Scott Wolkenberg,Douglas Beshore,Joseph L Duffy, Christine C Chang,Robert W Myers,Daniel J Klein,James Fells, Kate Holloway,Jin Wu,Guoxin Wu,Bonnie J Howell,Richard J O Barnard,Joseph Kozlowski

Bioorganic & Medicinal Chemistry Letters（2020）

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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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关键词

HDAC inhibitor,HIV latency,Zinc binding group,Shock and kill,2C4 cells,HDACs 1, 2, 3,HDACs 6, 8,HIV latency reversing agent

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