Facile synthesis and biological evaluation of chrysin derivatives

Omonga, Nicholas; Zia, Zakia; Ghanbour, Hesham; Ragazzon-Smith, Abby; Foster, Howard; Hadfield, John; Ragazzon, Patricia

Abstract

In this paper, novel synthetic methods, including microwave O-alkylation, were used to produce several chrysin derivatives. These compounds were purified, characterised and tested on different cell lines and bacterial strains. From this family, 7-(2,4-dinitrophenoxy)-5-hydroxy-3-phenyl-4H-chromen-4-one (C3) was shown to be extremely active on bacterial strains methicillin-resistant Staphylococcus aureus, Pseudomonas aeruginosa and Klebsiella pneumoniae as well as having anticancer activity on a range of cancer cell lines with IC50 values less than 30?µM. Chrysin has been known for their anticancer and antimicrobial properties, and this study not only corroborates this but also shows that it is possible to synthesise new improved derivatives with therapeutic possibilities.

Citation

Omonga, N., Zia, Z., Ghanbour, H., Ragazzon-Smith, A., Foster, H., Hadfield, J., & Ragazzon, P. (2021). Facile synthesis and biological evaluation of chrysin derivatives. Journal of Chemical Research, 1083-1092. https://doi.org/10.1177/17475198211057467

• Journal Article Type: Article
• Acceptance Date: Oct 18, 2021
• Publication Date: Nov 29, 2021
• Journal: Journal of Chemical Research
• Print ISSN: 1747-5198
• Publisher: SAGE Publications
• Peer Reviewed: Peer Reviewed
• Pages: 1083-1092
• DOI: https://doi.org/10.1177/17475198211057467
• Keywords: antibacterial; antifungal; chrysin derivatives; cytotoxicity; microwave
• Publisher URL: https://journals.sagepub.com/doi/10.1177/17475198211057467