Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives.
Serdar BurmaogluDerya Aktas AnilArzu GobekDeryanur KilicDerya YetkinNizami DuranOztekin AlgulPublished in: Journal of biomolecular structure & dynamics (2020)
A series of new chalcones containing fluoro atom at B ring have been designed, synthesized, and evaluated to be antiproliferative activity against a panel of human tumor cell lines. Some of the analogs (8, 9, 12, 45, 46 and 48) displayed powerful antiproliferative effects to certain human tumor cells, but all of them were devoid of any cytotoxicity towards the normal HEK 293. Acridine orange staining data supported that the cytotoxic and antiproliferative effects of the synthesized analogs on tumor cells are mediated through apoptosis. The compounds 12 and 46 manifested concentration-dependent antiproliferative activity in human hepatocellular carcinoma cell lines using an xCELLigence assay. The structures and antiproliferative activity relationship were further supported by in silico molecular docking study of the compounds against tubulin protein which suggests our compounds interference to cell division. Communicated by Ramaswamy H. Sarma.
Keyphrases
- molecular docking
- endothelial cells
- induced pluripotent stem cells
- pluripotent stem cells
- molecular dynamics simulations
- oxidative stress
- endoplasmic reticulum stress
- cell proliferation
- high resolution
- cell death
- mesenchymal stem cells
- bone marrow
- big data
- mass spectrometry
- cell cycle arrest
- binding protein
- protein protein
- amino acid
- electron transfer