Combining the platinum(II) drug candidate kiteplatin with 1,10-phenanthroline analogues
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.
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Pages, B. J., Sakoff, J., Gilbert, J., Zhang, Y., Kelly, S. M., Hoeschele, J. D., & Aldrich-Wright, J. R. (2018). Combining the platinum(II) drug candidate kiteplatin with 1,10-phenanthroline analogues. Dalton Transactions, 47(7), 2156–2163. https://doi.org/10.1039/C7DT04108J