ISBN: 978-83-60043-10-3 - eurobic9

Eurobic9, 2-6 September, 2008, Wrocław, Poland
P9. Synthesis, Structural Characterization, DNA Reactivity and
Antiproliferative Behaviour of cis/trans Ruthenium(II) Compounds
F. Barragán a , M. Montaña a , M. Prieto b , V. Moreno a , V. Noe c , C. Ciudad c , H. Garcia d
a
Inorganic Chemistry, University of Barcelona, Martí i Franquès 1-11, 08028, Barcelona, Spain
e-mail: flavia.barragan@qi.ub.es
b
Microbiology, University of Barcelona, Diagonal 645, 08028, Barcelona, Spain
c
Biochemistry and Molecular Biology (Pharmacy), University of Barcelona, Diagonal 643, 08028, Barcelona,
Spain
d
Chemistry, University of Lisbon, Campo Grande, 1749-016, Lisbon, Portugal
The platinum anti-tumour compounds era began with the cisplatin fortuitous finding by Rosenberg[1] and has
slowly opened the door to the new ruthenium compounds age. Some of them have successfully reached the final
stages of the clinic phases and others have shown promising anti-tumour activity. The insignificant side effects
of these compounds in comparison with those of platinum compounds and their anti-metastatic behaviour have
been the motor behind the rapid and extensive growth of this research field[2].
The synthesis of two new isomers are presented here; cis and trans complexes of ruthenium(II) with
thieno[3, 2-e][1]benzothiophene-2-carbonitrile (tbc) and 1, 2-Bis(diphenylphosphino)ethane, (dppe). The
compounds were characterized by spectroscopic analysis ( 1 H and 31 P NMR) and x-ray diffraction. The
interaction with DNA was studied by electrophoretic mobility and atomic force microscopy (AFM).
"In vitro" antiproliferative assays were carried out with three different tumour cell lines: HeLa (cervix), MiaPaca
(pancreas) and LoVo (colon). Although both isomers, cis and trans exhibit a remarkable anti-proliferative
activity against the three cell lines assayed (HeLa cell line: isomer cis IC50 (µM)=1.23, trans 0.77; MiaPaca cell
line: isomer cis IC50(µM) = 1.6, trans IC50(µM) = 0.4; LoVo cell line: isomer cis IC50(µM) = 1.5, trans IC50(µM)
= 0.9) the isomer with trans geometry has shown to be more active than the cis isomer.
References:
[1] B.Rosenberg, L. Van Camp, T. Trigas, Inhibition of cell division in E. Coli by electrolysis products from a
platinum electrode, Nature 205, 698-699 (1965)
[2] W.H. Ang, P.J.Dyson, Classical and Non-classical Ruthenium-based Anticancer Drugs: Towards Targeted
Chemotherapy (review), Eur. J. Inorg. Chem. 20, 4003-4018 (2006)
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