Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Bioorg Med Chem Lett
; 47: 128168, 2021 09 01.
Article
en En
| MEDLINE
| ID: mdl-34091041
A series of unique macrocyclic HDACs 1, 2, and 3 selective inhibitors were identified with good enzymatic activity and high selectivity over HDACs 6 and 8. These macrocyclic HDAC inhibitors used an ethyl ketone as the zinc-binding group. Compounds 25 and 26 stood out as leads due to their low double-digit nM EC50s in the 2C4 cell-based HIV latency reactivation assay. The PK profiles of these macrocyclic HDAC inhibitors still needed improvement.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
VIH
/
Fármacos Anti-VIH
/
Descubrimiento de Drogas
/
Inhibidores de Histona Desacetilasas
/
Histona Desacetilasas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2021
Tipo del documento:
Article