Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
Bioorg Med Chem
; 25(17): 4579-4594, 2017 09 01.
Article
en En
| MEDLINE
| ID: mdl-28739157
ABSTRACT
A series of cycloalkyl substituted analogues of the natural product sinefungin lacking the amino-acid moiety was designed and synthesized. Two stereoisomers (6-R and 6-S) were separated and their bioactivities examined against EHMT1/2. Of which, compound 14d showed an inhibitory activity against EHMT1/2 (88.9%, IC50=21.8µM for EHMT1 and 77.6%, IC50=39.6µM for EHMT2, respectively) similar to that of sinefungin (100.0%, IC50=28.4µM for EHMT1 and 79.5%, IC50=30.1µM for EHMT2, respectively). Further studies against other methyltransferases such as PRMT1 showed no activity except that 12d displayed about 20% inhibition.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Adenosina
/
N-Metiltransferasa de Histona-Lisina
/
Inhibidores Enzimáticos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2017
Tipo del documento:
Article
País de afiliación:
China