Facile synthesis and biological evaluation of chrysin derivatives

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

doi:10.1177/17475198211057467

Facile synthesis and biological evaluation of chrysin derivatives

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

Authors

Nicholas Omonga

Zakia Zia

Hesham Ghanbour

Abby Ragazzon-Smith

Howard Foster

John Hadfield

Patricia Ragazzon p.ragazzon@keele.ac.uk

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.

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