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

Pages, B. J., Sakoff, J., Gilbert, J., Zhang, Y., Kelly, S. M. , Hoeschele, J. D. and Aldrich-Wright, J. R. (2018) Combining the platinum(ii) drug candidate kiteplatin with 1,10-phenanthroline analogues. Dalton Transactions, 47(7), pp. 2101-2472. (doi:10.1039/c7dt04108j) (PMID:29192713)

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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.

Item Type:Articles
Additional Information:We thank Western Sydney University for providing financial support through internal research grants. B. J. P. was supported by an Australian Postgraduate Award and a Western Sydney University Top-Up Award.
Keywords:Inorganic chemistry.
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Kelly, Dr Sharon
Authors: Pages, B. J., Sakoff, J., Gilbert, J., Zhang, Y., Kelly, S. M., Hoeschele, J. D., and Aldrich-Wright, J. R.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
Journal Name:Dalton Transactions
Publisher:Royal Society of Chemistry
ISSN:1477-9226
ISSN (Online):1477-9234
Published Online:27 November 2017
Copyright Holders:Copyright © 2018 The Royal Society of Chemistry
First Published:First published in Dalton Transactions 47(7):2101-2472
Publisher Policy:Reproduced in accordance with the copyright policy of the publisher

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