Synthesis and analysis of the structure, diffusion and cytotoxicity of heterocyclic platinum(IV) complexes

Freddy J. Macias, Krishant M. Deo, Benjamin J. Pages, Paul Wormell, Jack K. Clegg, Yingjie Zhang, Feng Li, Gang Zheng, Jennette Sakoff, Jayne Gilbert, Janice R. Aldrich-Wright

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    30 Citations (Scopus)

    Abstract

    We have developed six dihydroxidoplatinum(IV) compounds with cytotoxic potential. Each derived from active platinum(II) species, these complexes consist of a heterocyclic ligand (HL) and ancillary ligand (AL) in the form [Pt(HL)(AL)(OH)2]2+, where HL is a methyl-functionalised variant of 1,10-phenanthroline and AL is the S,S or R,R isomer of 1,2-diaminocyclohexane. NMR characterisation and X-ray diffraction studies clearly confirmed the coordination geometry of the octahedral platinum(IV) complexes. The self-stacking of these complexes was determined using pulsed gradient stimulated echo nuclear magnetic resonance. The self-association behaviour of square planar platinum(II) complexes is largely dependent on concentration, whereas platinum(IV) complexes do not aggregate under the same conditions, possibly due to the presence of axial ligands. The cytotoxicity of the most active complex, exhibited in several cell lines, has been retained in the platinum(IV) form.
    Original languageEnglish
    Pages (from-to)16990-17001
    Number of pages12
    JournalChemistry: A European Journal
    Volume21
    Issue number47
    DOIs
    Publication statusPublished - 2015

    Keywords

    • X-ray diffraction
    • antineoplastic agents
    • cancer
    • cytotoxicity
    • platinum

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