Autor(en)
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
Teil von
  • Bioorganic & medicinal chemistry letters, 2020-07-01, Vol.30 (13), p.127197
Ort / Verlag
England
Links zum Volltext
Beschreibungen
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.
Format
Sprache(n)
Englisch
Identifikator(en)
ISSN: 1464-3405
Links zum Inhalt
Schlagwörter
Systemstelle
Signatur

Weiterführende Literatur

Empfehlungen zum selben Thema automatisch vorgeschlagen von bX
Die Universität der Informationsgesellschaft