Details

Autor(en) / Beteiligte

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

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2020-07, Vol.30 (13), p.127197-127197, Article 127197

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2020

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• [Display omitted] 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.