Synthesis and In Vitro Anticancer Evaluation of Flavone-1,2,3-Triazole Hybrids

Alexandra Németh-Rieder; Péter Keglevich; Attila Hunyadi; Ahmed Dhahir Latif; István Zupkó; László Hazai

doi:10.3390/molecules28020626

Synthesis and In Vitro Anticancer Evaluation of Flavone-1,2,3-Triazole Hybrids

Molecules. 2023 Jan 7;28(2):626. doi: 10.3390/molecules28020626.

Authors

Alexandra Németh-Rieder¹, Péter Keglevich¹, Attila Hunyadi², Ahmed Dhahir Latif^{3

4}, István Zupkó³, László Hazai¹

Affiliations

¹ Department of Organic Chemistry and Technology, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3., H-1111 Budapest, Hungary.
² Institute of Pharmacognosy, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary.
³ Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
⁴ Department of Pharmacology and Toxicology, Faculty of Medicine, Wasit University, Wasit 52001, Iraq.

Abstract

Hybrid compounds of flavones, namely chrysin and kaempferol, and substituted 1,2,3-triazole derivatives, were synthesized by click reaction of the intermediate O-propargyl derivatives. 4-Fluoro- and 4-nitrobenzyl-1,2,3-triazole-containing hybrid molecules were prepared. The mono- and bis-coupled hybrids were investigated on 60 cell lines of 9 common cancer types (NCI60) in vitro as antitumor agents. Some of them proved to have a significant antiproliferative effect.

Keywords: 1,2,3-triazole; anticancer activity; chrysin; flavones; hybrids; kaempferol.

MeSH terms

Antineoplastic Agents* / pharmacology
Cell Line, Tumor
Cell Proliferation
Drug Screening Assays, Antitumor
Flavones* / pharmacology
Molecular Structure
Structure-Activity Relationship
Triazoles / pharmacology

Substances

Triazoles
Antineoplastic Agents
Flavones

Grants and funding

This research received no external funding.