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Type: Journal article
Title: X-ray fluorescence imaging of single human cancer cells reveals that the N-heterocyclic ligands of iodinated analogues of ruthenium anticancer drugs remain coordinated after cellular uptake
Author: Antony, S.
Aitken, J.
Vogt, S.
Lai, B.
Brown, T.
Spiccia, L.
Harris, H.
Citation: Journal of Biological Inorganic Chemistry, 2013; 18(7):845-853
Publisher: Springer-Verlag
Issue Date: 2013
ISSN: 0949-8257
Statement of
Sumy Antony, Jade B. Aitken, Stefan Vogt, Barry Lai, Tracey Brown, Leone Spiccia, Hugh H. Harris
Abstract: Analogues of KP1019 containing iodinated indazole ligands were prepared to investigate the biological fate of the Ru-N-heterocycle bond in this class of anticancer agents. The new complexes, 5-iodoindazolium trans-tetrachloridobis(5-iodoindazole)ruthen(III)ate (1) and 5-iodoindazolium trans-tetrachlorido(dimethyl sulfoxide)(5-iodoindazole)ruthen(III)ate (3), were characterized by elemental analysis, mass spectrometry and UV-vis spectrophotometry. Tetramethylammonium salts of these complexes (2 and 4) were synthesized and characterized in a similar manner. Half-maximum inhibitory concentrations of 2 and 4 with regard to A549 cells at 24 h were determined on the basis of the dose-response curves derived from real-time cell adhesion impedance measurements and were shown to be in the same range as those determined for KP1019 and NAMI-A using the same method. X-ray fluorescence imaging of single cultured A549 cells treated with 2 or 4 showed that, in both cases, the distribution of ruthenium and iodine was identical, indicating that the Ru-N bonds in the anionic complexes remained intact after incubation in culture medium and subsequent cellular uptake and processing.
Keywords: Anticancer drugs; Ruthenium; Iodine; X-ray fluorescence imaging
Rights: © SBIC 2013
RMID: 0020131817
DOI: 10.1007/s00775-013-1027-z
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Appears in Collections:Chemistry and Physics publications

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