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Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
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.
  • Yu W; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: wensheng.yu@merck.com.
  • Liu J; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Yu Y; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Zhang V; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Clausen D; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kelly J; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Wolkenberg S; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Beshore D; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Duffy JL; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Chung CC; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Myers RW; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Klein DJ; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Fells J; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Holloway K; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Wu J; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Wu G; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Howell BJ; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Barnard RJO; Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
  • Kozlowski J; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 30(13): 127197, 2020 07 01.
Article en En | MEDLINE | ID: mdl-32331932
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.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Activación Viral / VIH-1 / Latencia del Virus / Fármacos Anti-VIH / Inhibidores de Histona Desacetilasas / Cetonas Límite: Animals / Humans Idioma: En Año: 2020 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Activación Viral / VIH-1 / Latencia del Virus / Fármacos Anti-VIH / Inhibidores de Histona Desacetilasas / Cetonas Límite: Animals / Humans Idioma: En Año: 2020 Tipo del documento: Article