Design, synthesis and bioevaluation of novel prenylated chalcones derivatives as potential antitumor agents.
Eur J Pharm Sci
; 192: 106660, 2024 Jan 01.
Article
in En
| MEDLINE
| ID: mdl-38052256
ABSTRACT
A series of novel prenylated chalcone derivatives with broad spectrum anticancer potential were designed and synthesized. Some of the synthesized target compounds showed potent anti-proliferative activities toward LNCaP (prostate cancer cell line), K562 (human leukemia cells), A549 (human lung carcinoma cell line) and HeLa (cervical cancer cell line) cell lines. Among of the active compounds, (E)-1-(4-(2-(diethylamino)ethoxy)-2-hydroxy-6-methoxy-3-(3-methylbut-2-en-1-yl)phenyl)-3-(pyridin-3-yl)prop-2-en-1-one (C36) was directly interacted with protein kinase B (PKB), also known as AKT, significantly inhibited the pPI3K, pAKT(Ser473) protein levels to repress the growth of cancer cells by inducing apoptosis, arresting cell cycle. Our studies provide support for prenylated chalcone derivatives potential applications in cancer treatment as a potential AKT inhibitor.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Chalcone
/
Chalcones
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Eur J Pharm Sci
Journal subject:
FARMACIA
/
FARMACOLOGIA
/
QUIMICA
Year:
2024
Document type:
Article
Affiliation country:
China