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Issue 5, 2011
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Copper complexes of bis(thiosemicarbazones): from chemotherapeutics to diagnostic and therapeutic radiopharmaceuticals

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Abstract

The molecules known as bis(thiosemicarbazones) derived from 1,2-diones can act as tetradentate ligands for Cu(II), forming stable, neutral complexes. As a family, these complexes possess fascinating biological activity. This critical review presents an historical perspective of their progression from potential chemotherapeutics through to more recent applications in nuclear medicine. Methods of synthesis are presented followed by studies focusing on their potential application as anti-cancer agents and more recent investigations into their potential as therapeutics for Alzheimer's disease. The Cu(II) complexes are of sufficient stability to be used to coordinate copper radioisotopes for application in diagnostic and therapeutic radiopharmaceuticals. Detailed understanding of the coordination chemistry has allowed careful manipulation of the metal based properties to engineer specific biological activities. Perhaps the most promising complex radiolabelled with copper radioisotopes to date is CuII(atsm), which has progressed to clinical trials in humans (162 references).

Graphical abstract: Copper complexes of bis(thiosemicarbazones): from chemotherapeutics to diagnostic and therapeutic radiopharmaceuticals

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Publication details

The article was received on 17 Dec 2010, published on 15 Mar 2011 and first published online on 15 Mar 2011


Article type: Critical Review
DOI: 10.1039/C0CS00215A
Citation: Chem. Soc. Rev., 2011,40, 3005-3018
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    Copper complexes of bis(thiosemicarbazones): from chemotherapeutics to diagnostic and therapeutic radiopharmaceuticals

    B. M. Paterson and P. S. Donnelly, Chem. Soc. Rev., 2011, 40, 3005
    DOI: 10.1039/C0CS00215A

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