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Issue 17, 2010
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Non-classical anticancer agents: synthesis and biological evaluation of zinc(ii) heteroleptic complexes

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Abstract

New heteroleptic complexes (1–8) containing Zn(II) ion coordinated to an N,N-chelating ligand (the 4,4′-dinonyl-2,2′-bipyridine, bpy-9) and to diketonates L such as tropoloids (Tropolone and Hinokitiol) or 1-phenyl-3-methyl-4-R-5-pyrazolones have been synthesized by using different stoichiometric ratio with respect to the L ancillary ligand. The molecular structure of the bis-tropolonate derivative [(bpy-9)Zn(L)2] 5 has been determined by single-crystal X-ray diffraction. The antitumour activity of all Zn(II) complexes was tested in vitro against three different human prostate cancer cells: DU145, LNCaP and PC-3. Moreover, their effect on cell survival signalling and/or inhibitors of the PC-3 cell cycle have been analyzed. The results indicate that 1–8 exhibit strong cytotoxic activity against all cell lines affecting key molecules such as p-AKT and p21 waf, involved in the cell proliferation and/or arrest. Zinc(II) is thus a promising alternative to Pt(II) ion in the design of new, better performing antitumour agents.

Graphical abstract: Non-classical anticancer agents: synthesis and biological evaluation of zinc(ii) heteroleptic complexes

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Publication details

The article was received on 22 Oct 2009, accepted on 03 Mar 2010 and first published on 24 Mar 2010


Article type: Paper
DOI: 10.1039/B922101H
Dalton Trans., 2010,39, 4205-4212

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    Non-classical anticancer agents: synthesis and biological evaluation of zinc(II) heteroleptic complexes

    P. F. Liguori, A. Valentini, M. Palma, A. Bellusci, S. Bernardini, M. Ghedini, M. L. Panno, C. Pettinari, F. Marchetti, A. Crispini and D. Pucci, Dalton Trans., 2010, 39, 4205
    DOI: 10.1039/B922101H

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