Facile synthesis and biological evaluation of chrysin derivatives

Omonga, NF; Zia, Z; Ghanbour, HA; Ragazzon-Smith, AH; Foster, HA; Hadfield, JA; Ragazzon, PA

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, 45(11-12), 1083-1092. https://doi.org/10.1177/17475198211057467

• Journal Article Type: Article
• Online Publication Date: Nov 29, 2021
• Publication Date: Nov 29, 2021
• Deposit Date: Dec 6, 2021
• Publicly Available Date: Dec 6, 2021
• Journal: Journal of Chemical Research
• Print ISSN: 1747-5198
• Electronic ISSN: 2047-6507
• Publisher: SAGE Publications
• Volume: 45
• Issue: 11-12
• Pages: 1083-1092
• DOI: https://doi.org/10.1177/17475198211057467
• Publisher URL: https://doi.org/10.1177/17475198211057467
• Related Public URLs: https://journals.sagepub.com/home/chl
• Additional Information: Funders : Nigerian Government;University of Salford; Projects : The synthesis, isolation and evaluation of novel anticancer and antibacterial therapeutics derived from natural products