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Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Clausen, Dane J; Liu, Jian; Yu, Wensheng; 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.
Afiliación
  • Clausen DJ; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: dane.clausen@merck.com.
  • Liu J; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Yu W; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, 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(17): 127367, 2020 09 01.
Article en En | MEDLINE | ID: mdl-32738976
The synthesis and SAR development of a trisubstituted imidazole HDAC inhibitor is described. The compounds were synthesized with high diastereocontrol by leveraging Ellman sulfinyl imine chemistry. Structural elucidation provided insight into binding mode and supported design rational. Pharmacokinetic properties of lead compounds were determined.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Inhibidores de Histona Desacetilasas / Histona Desacetilasas Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article
Texto completo
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PubMed Links
Buscar en Google

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Inhibidores de Histona Desacetilasas / Histona Desacetilasas Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article