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

* Corresponding authors

a Nanoscale Organisation and Dynamics Group, Western Sydney University, Campbelltown, NSW 2560, Australia
E-mail: J.Aldrich-Wright@westernsydney.edu.au

b Calvary Mater Newcastle, Waratah, NSW 2298, Australia

c Australian Nuclear Science and Technology Organisation, Locked Bag 2001, Kirrawee DC, NSW 2232, Australia

d Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, UK

e Department of Chemistry, Eastern Michigan University, Ypsilanti, MI 48197, USA

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 1_S,2_S_-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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Article information

DOI

https://doi.org/10.1039/C7DT04108J

Article type

Paper

Submitted

31 Oct 2017

Accepted

27 Nov 2017

First published

27 Nov 2017

Download Citation

Dalton Trans., 2018,47, 2156-2163

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