Background:
Cancer is one of the leading causes of morbidity and mortality worldwide, with approximately
14 million new cases in 2012, with most of the clinically used drugs being ineffective.
Methylxanthines have raised more interest in research on modifying their structure because of their diverse
biological activity. In addition, the piperazine nucleus is one of the most important heterocycles exhibiting remarkable
pharmacological activities.
Methods:
The structure of the obtained compounds was characterized and elucidated by IR, 1H and 13C NMR
and LCMS spectral analysis. The purity of the substances was proven by corresponding melting points and
elemental analysis. The antioxidant activity was evaluated by four common methods – DPPH, ABTS, FRAP and
lipid peroxidation assay. The cytotoxic effects of the tested series were evaluated using the standard MTT-dye
reduction assay on three tumour cell lines.
Results:
A series of new xanthine derivatives comprising an arylpiperazine moiety at N1 were synthesized. The
cytotoxicity against human T-cell leukemia cell SKW-3, human acute myeloid leukemia HL-60 and human Bcell
precursor leukemia cell REH was evaluated. The relationship between the structure and citotoxicity of the
compounds was investigated by quantitative structure-activity relationship (QSAR) analysis and the important
structural parameters were drawn.
Conclusion:
The highest antioxidant activity was demonstrated by compound 6c. The highest cytotoxic effect
was observed for compound 6f. It was found that cytotoxicity against SKW-3 depends on the electron density
distribution in the structures. Branching of the molecular skeleton and introduction of heteroatoms like fluorine
and sulfur in the structures also significantly improved the antiproliferative activity of the compounds.
Improving the Light Quality of White Light‐Emitting Diodes Using Cellulose Nanocrystal‐Filled Phosphors
