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.
Highlights
In the search for new drugs to overcome drug-resistant infections and cancers, phytochemicals have become the go-to source for inspiration
Microwave chemistry has been at the front of green chemistry synthetic methods as it allows for reduction of solvent used, time and electricity as well as making some reactions more favourable.[18]
O-alkylation in chrysin is favoured on position 7, this is due to the interaction between the carbonyl oxygen in position 4 and the hydroxyl in position 5.19 The proximity of these two groups allows the formation of hydrogen bonding which requires harsher conditions for O-alkylation
Summary
In the search for new drugs to overcome drug-resistant infections and cancers, phytochemicals have become the go-to source for inspiration. Isoprenoids serve as the backbone from which many phytochemicals are biosynthesised via the cytosolic mevalonate (MVA) and the 2C-methyl-D-erythritol-4-phosphate (MEP) pathways.[1] Some phytochemicals, like flavonoids, are synthesised via the phenylpropanoid pathway, they exhibit both. Journal of Chemical Research antimicrobial and anticancer activities.[2] The antimicrobial activity could be a result of impairment of the cell membrane integrity and cell agglutination.[3] The anticancer activity could be due to modulation of various mechanisms such as angiogenesis, apoptosis, metastasis, differentiation and cell proliferation.[4,5] The increase in research targeted at developing new drugs for cancer and infectious diseases has gained momentum in the last decades
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