Design, synthesis and biological evaluation of aloperine derivatives as potential anticancer agents.
J Asian Nat Prod Res
; 26(9): 1057-1086, 2024 Sep.
Article
en En
| MEDLINE
| ID: mdl-38920368
ABSTRACT
Modifications at different positions on the aloperine molecule were performed to improve its anticancer activity and develop anticancer drugs. The in vitro anticancer activities of 44 synthesized compounds were evaluated. The effect of modification positions on anticancer activity was discussed and a structure-activity relationship analysis was established. A novel series of compounds with modifications at the N12 position showed much higher cytotoxicity than aloperine. Among them, compound 22 displayed promising in vitro anticancer activity against PC9 cells with a median inhibitory concentration (IC50) of 1.43 µM. The mechanism studies indicated that compound 22 induced cell apoptosis and cell cycle arrest in PC9 cells. These results demonstrate the potential of aloperine thiourea derivatives in anticancer activity.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Piperidinas
/
Ensayos de Selección de Medicamentos Antitumorales
/
Apoptosis
/
Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
J Asian Nat Prod Res
Asunto de la revista:
BOTANICA
/
QUIMICA
Año:
2024
Tipo del documento:
Article
País de afiliación:
China