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Combining the platinum(II) drug candidate kiteplatin with 1,10-phenanthroline analogues

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Abstract

Platinum complexes of the type [Pt(PL)(AL)]2+ where PL is a derivative of 1,10-phenanthroline and AL is cis-1,4-diaminocyclohexane (1,4-dach), have been synthesised and characterised by ultraviolet spectroscopy, elemental microanalysis, nuclear magnetic resonance and X-ray crystallography. The calf-thymus DNA binding affinity of these complexes was determined by isothermal titration calorimetry, revealing higher DNA affinity than their 1S,2S-diaminocyclohexane analogues. In vitro cytotoxicity was assessed in eleven human cell lines, revealing unexpectedly low activity for the 1,4-dach complexes.

Graphical abstract: Combining the platinum(ii) drug candidate kiteplatin with 1,10-phenanthroline analogues

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Publication details

The article was received on 31 Oct 2017, accepted on 27 Nov 2017 and first published on 27 Nov 2017


Article type: Paper
DOI: 10.1039/C7DT04108J
Citation: Dalton Trans., 2018, Advance Article
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    Combining the platinum(II) drug candidate kiteplatin with 1,10-phenanthroline analogues

    B. J. Pages, J. Sakoff, J. Gilbert, Y. Zhang, S. M. Kelly, J. D. Hoeschele and J. R. Aldrich-Wright, Dalton Trans., 2018, Advance Article , DOI: 10.1039/C7DT04108J

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