Antony, S.Aitken, J.Vogt, S.Lai, B.Brown, T.Spiccia, L.Harris, H.2013-11-272013-11-272013Journal of Biological Inorganic Chemistry, 2013; 18(7):845-8530949-82571432-1327http://hdl.handle.net/2440/81327Analogues 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.en© SBIC 2013Anticancer drugsRutheniumIodineX-ray fluorescence imagingJournal article002013181710.1007/s00775-013-1027-z0003246362000112-s2.0-8488565536418019Harris, H. [0000-0002-3472-8628]