Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).
Bioorg Med Chem Lett
; 27(10): 2099-2101, 2017 05 15.
Article
en En
| MEDLINE
| ID: mdl-28390942
ABSTRACT
We report a series of tranylcypromine analogues containing a fluorine in the cyclopropyl ring. A number of compounds with additional m- or p-substitution of the aryl ring were micromolar inhibitors of the LSD1 enzyme. In cellular assays, the compounds inhibited the proliferation of acute myeloid leukemia cell lines. Increased levels of the biomarkers H3K4me2 and CD86 were consistent with LSD1 target engagement.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tranilcipromina
/
Inhibidores Enzimáticos
/
Histona Demetilasas
Límite:
Humans
Idioma:
En
Año:
2017
Tipo del documento:
Article