In Vitro and In Silico Evaluation of the Anticancer and Antiparasitic Activities of New 2‐Methoxy Azachalconium Bromides DOI
Mai F. AlSakhen, Sana I. Kanaan, Khaled Saleh

et al.

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(16)

Published: April 1, 2025

Abstract Three new N ‐alkylpyridinium‐based 2‐methoxy chalcones with long, fatty alkyl chains were prepared and tested for their anticancer antiparasitic activities. The ‐octadecyl derivative ( 2c ) displayed considerable activity against selectivity BRAF‐mutant HT‐29 colorectal carcinoma cells. Increased mRNA expression of caspases apoptosis induction was found. In addition, MEKs ERKs upregulated. EGFR inhibition identified as mechanism action this compound further supported by in silico molecular docking studies, which revealed a binding energy −9.19 kcal/mol EGFR. Additionally, strong affinity VEGFR‐2 observed −11.01 kcal/mol. development the described chalcone drug appears to be promising. all three derivatives exhibited significant activities Toxoplasma gondii Leishmania major parasites, albeit without selectivity. Thus, present study describes first time kinase‐inhibitory, anti‐leishmanial, anti‐toxoplasmal ‐alkyl azachalconium compounds.

Language: Английский

In Vitro and In Silico Evaluation of the Anticancer and Antiparasitic Activities of New 2‐Methoxy Azachalconium Bromides DOI
Mai F. AlSakhen, Sana I. Kanaan, Khaled Saleh

et al.

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(16)

Published: April 1, 2025

Abstract Three new N ‐alkylpyridinium‐based 2‐methoxy chalcones with long, fatty alkyl chains were prepared and tested for their anticancer antiparasitic activities. The ‐octadecyl derivative ( 2c ) displayed considerable activity against selectivity BRAF‐mutant HT‐29 colorectal carcinoma cells. Increased mRNA expression of caspases apoptosis induction was found. In addition, MEKs ERKs upregulated. EGFR inhibition identified as mechanism action this compound further supported by in silico molecular docking studies, which revealed a binding energy −9.19 kcal/mol EGFR. Additionally, strong affinity VEGFR‐2 observed −11.01 kcal/mol. development the described chalcone drug appears to be promising. all three derivatives exhibited significant activities Toxoplasma gondii Leishmania major parasites, albeit without selectivity. Thus, present study describes first time kinase‐inhibitory, anti‐leishmanial, anti‐toxoplasmal ‐alkyl azachalconium compounds.

Language: Английский

Citations

0