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Bis‐ and Tris(carboxylato)platinum(IV) Complexes with Mixed Am(m)ine Ligands in the trans Position Exhibiting Exceptionally High Cytotoxicity
Author(s) -
Hoffmeister Björn R.,
Hejl Michaela,
Jakupec Michael A.,
Galanski Mathea Sophia,
Keppler Bernhard K.
Publication year - 2015
Publication title -
european journal of inorganic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.667
H-Index - 136
eISSN - 1099-0682
pISSN - 1434-1948
DOI - 10.1002/ejic.201403226
Subject(s) - chemistry , bromide , cytotoxicity , cisplatin , stereochemistry , carboxylate , tris , nuclear magnetic resonance spectroscopy , platinum , medicinal chemistry , in vitro , inorganic chemistry , organic chemistry , biochemistry , medicine , catalysis , surgery , chemotherapy
A series of seven diam(m)inebis(carboxylato)dihydroxidoplatinum(IV) and eleven diam(m)inetris(carboxylato)hydroxidoplatinum(IV) complexes with am(m)ine ligands in the trans position was synthesized and characterized by multinuclear 1 H, 13 C, 15 N, 195 Pt NMR spectroscopy. IC 50 values for all eighteen substances were determined by means of the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl‐2 H ‐tetrazolium bromide (MTT) assay for three human cancer cell lines. In cisplatin‐sensitive CH1(PA‐1) cancer cells, diam(m)inebis(carboxylato)dihydroxidoplatinum(IV) complexes displayed 50 % inhibitory concentrations in the micromolar range, whereas for the most lipophilic compounds of the diam(m)inetris(carboxylato)hydroxidoplatinum(IV) series, promising IC 50 values in the nanomolar range were found.