Discovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin.
J Enzyme Inhib Med Chem
; 33(1): 1199-1211, 2018 Dec.
Article
en En
| MEDLINE
| ID: mdl-30132373
ABSTRACT
A series of new trimethoxyphenyl-4H-chromen derivatives as telomerase inhibitors through regulation dyskerin were designed and synthesised. The anticancer activity assay in vitro showed that compound 5i 3-(4-(4-isonicotinoylpiperazin-1-yl)butoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one exhibited high activity against Hela, SMMC-7721, SGC-7901, U87 and HepG2 cell lines. Compound 5i also showed potent inhibitory activity against telomerase. The further results confirmed this title compound could significantly improve pathological changes induced rat hepatic tumor in vivo. Preliminary mechanisms showed that compound 5i inhibited telomerase activity through decrease expression of dyskerin.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Proteínas Nucleares
/
Cromanos
/
Proteínas de Ciclo Celular
/
Telomerasa
/
Inhibidores Enzimáticos
/
Descubrimiento de Drogas
/
Antineoplásicos
Límite:
Animals
/
Female
/
Humans
/
Male
Idioma:
En
Revista:
J Enzyme Inhib Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2018
Tipo del documento:
Article