Back to Search
Start Over
Efficient synthesis and evaluation of therapeutic potential of fluorine containing 2-arylchromen-4-ones.
- Source :
-
Molecular diversity [Mol Divers] 2024 Jul 16. Date of Electronic Publication: 2024 Jul 16. - Publication Year :
- 2024
- Publisher :
- Ahead of Print
-
Abstract
- A large series of 2-arylchromen-4-ones containing from 1 to 3 fluorine atoms or a trifluoromethyl group in the structure was synthesized by condensation of fluorinated 2-hydroxyacetophenones with benzaldehydes in an alkaline medium and subsequent oxidative cyclization of the resulting 2'-hydroxychalcones by action of I <subscript>2</subscript> in DMSO. The cytotoxicity of the obtained compounds was studied in glioblastoma cell line, SNB19, and in a monkey-derived normal kidney epithelium cell line, Vero. In addition, antiglycation activity of the obtained compounds was evaluated. The inhibitory activity of some fluorinated 2-arylchromen-4-ones against acetylcholinesterase, butyrylcholinesterase and carboxylesterase as well their primary antioxidant activity in ABTS and FRAP tests were investigated. Screening of the synthesized compounds for their inhibitory activity against influenza A virus A/Puerto Rico/8/34 (H1N1) in the MDCK cell culture revealed that fluorinated compounds 32, 31 and 39 showed manifest antiviral effects (with IS = 57, 38 and 25 correspondingly) that makes this series of new biologically attractive fluorinated heterocycles promising for further development and in-depth study.<br /> (© 2024. The Author(s), under exclusive licence to Springer Nature Switzerland AG.)
Details
- Language :
- English
- ISSN :
- 1573-501X
- Database :
- MEDLINE
- Journal :
- Molecular diversity
- Publication Type :
- Academic Journal
- Accession number :
- 39012566
- Full Text :
- https://doi.org/10.1007/s11030-024-10925-6