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Updated: Dec 23, 2025

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High Throughput In Vitro Assessment of Latency Reversing Agents on HIV Transcription and Splicing
Published on: January 22, 2019
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Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation
Wensheng Yu1, Jian Liu1, Younong Yu1
1Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorganic & Medicinal Chemistry Letters
|April 26, 2020
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.
Keywords:
2C4 cellsHDAC inhibitorHDACs 1, 2, 3HDACs 6, 8HIV latencyHIV latency reversing agentShock and killZinc binding group
