Metallomics, 2013, 5, 973–987. DOI: 10.1039/c3mt00128h

Synthesis of [PtCl2(4,4′-dialkoxy-2,2′-bipyridine)] complexes and their in vitro anticancer properties.

Van Vo, Ontida Tanthmanatham, Haesook Han, Pradip K. Bhowmik and Bryan L. Spangelo

Department of Chemistry, University of Nevada Las Vegas, 4505 S. Maryland Parkway, Box 454003, Las Vegas, NV 89154-4003, USA. E-mail: bryan.spangelo@unlv.edu, pradip.bhowmik@unlv.edu

 

ABSTRACT

A series of [Pt(II)Cl2(4,4′-dialkoxy-2,2′-bipyridine)] complexes of the general formula of [Pt(II)Cl2(4,4′-bis(RO)-2,2′-bipyridine)] (where R = -(CH2)n-1CH3, n = 2-6,8) were synthesized and characterized using 1H NMR, 13C NMR spectroscopy, elemental analysis, mass spectroscopy, and differential scanning calorimetry measurements.  The in vitro anti-proliferative activities of these compounds were evaluated against human cancer cell lines A549 (lung adenocarcinoma), DU145 (prostate carcinoma), MCF-7 (breast adenocarcinoma), and MDA-MB-435 (melanoma) using the MTS cell proliferation assay. Several Pt (II) coordination compounds were found to have greatly enhanced activity compared to cisplatin after a one hour treatment in all cell lines tested. A structure-activity relationship was observed, that is, the activity increases as the carbon chain length of the alkyl group increases.  The activity was maximum when the carbon chain length reaches four or five carbons and decreased with the longer carbon chain length.  Fluorescence microscopy and flow cytometry data indicate that the main mode of cell death is through apoptosis with some necrotic responses.

PMID: 23817622

Bryan L. Spangelo -fig1

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