Design, synthesis and antiproliferative screening of newly synthesized acrylate derivatives as potential anticancer agents.
RSC Adv
; 13(34): 23538-23546, 2023 Aug 04.
Article
en En
| MEDLINE
| ID: mdl-37546218
ABSTRACT
A new series of acrylic acid and acrylate ester derivatives as modified analogs of tubulin polymerization inhibitors were designed and synthesized. The antiproliferative activity of the constructed molecules was investigated against MCF-7 breast carcinoma cells using CA-4 as positive molecule. Methyl acrylate ester 6e emerged as the most potent cytotoxic agent against MCF-7 cells, with an IC50 value of 2.57 ± 0.16 µM. Also, methyl acrylate ester molecule 6e showed good ß-tubulin polymerization inhibition activity. Cellular cycle analysis showed that compound 6e can arrest MCF-7 cells at the G2/M phase. In addition, this compound produced a significant increase in apoptotic power as compared to control untreated MCF-7 cells. Furthermore, the effect of acrylate ester 6e on the gene expression levels of p53, Bax and Bcl-2 was investigated. This molecule increased the expression levels of both p53 and Bax, and decreased the gene expression level of Bcl-2 as compared to control untreated MCF-7 carcinoma cells.
Texto completo:
1
Colección:
01-internacional
Tipo de estudio:
Diagnostic_studies
/
Screening_studies
Idioma:
En
Revista:
RSC Adv
Año:
2023
Tipo del documento:
Article