On the basis of the urgent need to develop innovative and safe anticancer compounds, a series of chalcones, functionalized with various substituents in the aromatic portions and a long N-alkyl amide moiety, were designed and synthesized. The compatibility of novel compounds was firstly evaluated on non-tumoral human gingival fibroblasts (HGFs), secondly, the anti-proliferative effect on an adenocarcinoma gastric cell line (AGS) was measured. Among the chalcones, compound 3, at 50 µM after 48 and 72 h, showed, at the same time, an appreciable capability to counteract tumoral AGS viability and to preserve a high rate of healthy HGFs viability. Cell cycle analysis, performed on AGS cell line with 3 subtoxic dose (30 µM), suggested that the anti-proliferative effect could be related to a cell cycle arrest during the first stage and to an increase in the oxidative stress demonstrated by the significant augmentation of Reactive Oxygen Species release. Collectively, we have demonstrated that chalcone 3 had a potent anti-proliferative potential for the treatment of gastric adenocarcinoma and could be further investigated for new drug development.

Integrating N-alkyl amide in the chalcone framework: synthesis and evaluation of its anti-proliferative potential against AGS cancer cell line

Zara S.
Co-primo
;
Ricci A.;Carradori S.
Ultimo
2023-01-01

Abstract

On the basis of the urgent need to develop innovative and safe anticancer compounds, a series of chalcones, functionalized with various substituents in the aromatic portions and a long N-alkyl amide moiety, were designed and synthesized. The compatibility of novel compounds was firstly evaluated on non-tumoral human gingival fibroblasts (HGFs), secondly, the anti-proliferative effect on an adenocarcinoma gastric cell line (AGS) was measured. Among the chalcones, compound 3, at 50 µM after 48 and 72 h, showed, at the same time, an appreciable capability to counteract tumoral AGS viability and to preserve a high rate of healthy HGFs viability. Cell cycle analysis, performed on AGS cell line with 3 subtoxic dose (30 µM), suggested that the anti-proliferative effect could be related to a cell cycle arrest during the first stage and to an increase in the oxidative stress demonstrated by the significant augmentation of Reactive Oxygen Species release. Collectively, we have demonstrated that chalcone 3 had a potent anti-proliferative potential for the treatment of gastric adenocarcinoma and could be further investigated for new drug development.
File in questo prodotto:
File Dimensione Formato  
s11164-022-04864-w.pdf

Solo gestori archivio

Tipologia: PDF editoriale
Dimensione 1.26 MB
Formato Adobe PDF
1.26 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11564/793152
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 2
  • ???jsp.display-item.citation.isi??? 4
social impact