Published October 1, 2021 | Version v.1
Journal article Restricted

Antitumor activity, DNA and BSA interactions of novel copper(II) complexes with 3,4-dihydro-2(1H)-quinoxalinones

Authors/Creators

  • 1. University of Kragujevac, Faculty of Science, Department of Chemistry, Radoja Domanovica 12, Kragujevac, Serbia
  • 2. University of Kragujevac, Institute for Information Technologies Kragujevac, Department of Sciences, Jovana Cvijića bb, 34000, Kragujevac, Serbia
  • 3. Institute for Oncology and Radiology of Serbia, Pasterova 14, 11000, Belgrade, Serbia
  • 4. Laboratory for Radiobiology and Molecular Genetics, Department of Health and Environment, "VINČA" Institute of Nuclear Sciences -National Institute of the Republic of Serbia, University of Belgrade, Mike Petrovica Alasa 12-14, Serbia

Description

Abstract

In order to discover new therapeutically active agents a series of novel copper(II) complexes with 3,4-dihydro-2(1H)-quinoxalinones were synthesized. All complexes were characterized by IR and EPR spectroscopic techniques and examined for their cytotoxic effect on human cancer cell lines HeLa, LS174, A549 and normal fibroblasts (MRC-5). For further examination of the cytotoxic mechanisms of novel complexes, three of them were chosen for analysing their effects on the distribution of HeLa cells in the cell cycle phases. The results of the flow cytometry analysis suggest that tested complexes lead to time-dependent accumulation of the cells in S and G2/M phases. The strongest accumulation effect showed complex 2d after 48 h of incubation. Competitive experiments with ethidium bromide (EB) indicated that tested compound 2d have affinity to displace EB from the EB-DNA complex through intercalation. Also, the binding parameters values for 2d-BSA complex showed that a reversible 2d-BSA complex is formed and ligand 2d can be stored and carried by BSA.

Notes

The authors are grateful to the Ministry of Education, Science and Technological Development of the Republic of Serbia for financial support (Agreement No. 451-03-9/2021-14/200122 and 451-03-9/2021- 14/200378).

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Related works

Is documented by
https://www.sciencedirect.com/science/article/abs/pii/S0009279721002854 (URL)
Is part of
0009-2797 (ISSN)