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Issue 21, 2011
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Pt(II) complexes with bidentate and tridentate pyrazolyl-containing chelators: synthesis, structural characterization and biological studies

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Abstract

A series of four Pt(II) complexes anchored by bidentate or tridentate pyrazolyl-alkylamine chelators bearing different substituents at the azolyl rings has been prepared with the aim to assess their interest in the design of novel anticancer drugs. All complexes have been fully characterized by classical analytical methods and three of them were characterized also by X-ray diffraction analysis. Their solution behavior, together with lipophilicity measurements, cell uptake, antiproliferative properties, DNA interaction have been evaluated. Albeit all the complexes were less active than cisplatin on ovarian carcinoma A2780 cell line, greatly retained their activity in the cisplatin-resistant A2780cisR cell line and presented a lower resistance factor compared to cisplatin. Moreover, the Pt(II) complexes under investigation were less prone to undergo deactivation by glutathione, believed to be the major cellular target of cisplatin that inactivates the drug by binding to it irreversibly.

Graphical abstract: Pt(ii) complexes with bidentate and tridentate pyrazolyl-containing chelators: synthesis, structural characterization and biological studies

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Publication details

The article was received on 16 Dec 2010, accepted on 24 Mar 2011 and first published on 21 Apr 2011


Article type: Paper
DOI: 10.1039/C0DT01785J
Citation: Dalton Trans., 2011,40, 5781-5792
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    Pt(II) complexes with bidentate and tridentate pyrazolyl-containing chelators: synthesis, structural characterization and biological studies

    C. Francisco, S. Gama, F. Mendes, F. Marques, I. Cordeiro dos Santos, A. Paulo, I. Santos, J. Coimbra, E. Gabano and M. Ravera, Dalton Trans., 2011, 40, 5781
    DOI: 10.1039/C0DT01785J

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