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Synthesis, spectral characterization, DNA binding ability and anti-cancer screening of new acridine-based derivatives

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Abstract

In this study, a series of newly synthesized acridine derivatives, compounds 4, 6a, and 6b, are described and their biological activity on HL-60 cell lines is assessed using a number of different techniques. Binding studies were also performed between the derivatives and DNA in order to characterize the mechanism of the agents’ effect in more detail. The results of ultraviolet–visible absorption spectroscopy prove that the binding of derivatives 4, 6a, and 6b had occurred with a binding constant value of K = 3.5 × 104–4.0 × 104 M−1. These findings are indicative of a strong interaction between the derivatives and DNA, and this hypothesis is supported by the results of the fluorescence emission, linear dichroism, and viscometric assays.

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Acknowledgements

This study was supported by Slovak Research and Development Agency under contract VVCE-0001-07, VEGA grants No. 1/0001/13, and 1/0672/11 and MH CZ-DRO (UHHK, 00179906). The authors would like to thank Jana Kašpárkova and Viktor Brabec for their advice on LD measurement and viscometric techniques.

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Authors and Affiliations

  1. Department of Biochemistry, P. J. Šafárik University, Košice, Slovakia

    Othman M. Salem, Jana Janočková & Mária Kožurková

  2. Department of Organic Chemistry, Institute of Chemistry, P. J. Šafárik University, Košice, Slovakia

    Mária Vilková & Ján Imrich

  3. Biomedical Research Center, University Hospital Hradec Kralove, Hradec Kralove, Czech Republic

    Jana Janočková & Mária Kožurková

  4. Department of Cellular Biology, Faculty of Science, Institute of Biology and Ecology, P. J. Šafárik University, Košice, Slovakia

    Rastislav Jendželovský & Peter Fedoročko

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  1. Othman M. Salem
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Correspondence to Mária Kožurková.

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Salem, O.M., Vilková, M., Janočková, J. et al. Synthesis, spectral characterization, DNA binding ability and anti-cancer screening of new acridine-based derivatives. Med Chem Res 26, 2309–2321 (2017). https://doi.org/10.1007/s00044-017-1931-9

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  • DOI: https://doi.org/10.1007/s00044-017-1931-9

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