TY - JOUR
T1 - Unsymmetric mono- and dinuclear platinum(IV) complexes featuring an ethylene glycol moiety: Synthesis, characterization, and biological activity
AU - Pichler, Verena
AU - Heffeter, Petra
AU - Valiahdi, Seied Mojtaba
AU - Kowol, Christian
AU - Egger, Alexander
AU - Berger, Walter
AU - Jakupec, Michael
AU - Galanski, Mathea Sophia
AU - Keppler, Bernhard
N1 - Accession Number: WOS:000312681100019
PY - 2012
Y1 - 2012
N2 - Eight novel mononuclear and two dinuclear platinum(IV) complexes were synthesized and characterized by elemental analysis, one- and two-dimensional NMR spectroscopy, mass spectrometry, and reversed-phase HPLC (log kw) and in one case by X-ray diffraction. Cytotoxicity of the compounds was studied in three human cancer cell lines (CH1, SW480, and A549) by means of the MTT assay, featuring IC50 values to the low micromolar range. Furthermore a selected set of compounds was investigated in additional cancer cell lines (P31 and P31/cis, A2780 and A2780/cis, SW1573, 2R120, and 2R160) with regard to their resistance patterns, offering a distinctly different scheme compared to cisplatin. To gain further insights into the mode of action, drug uptake, DNA synthesis inhibition, cell cycle effects, and induction of apoptosis were determined for two characteristic substances.
AB - Eight novel mononuclear and two dinuclear platinum(IV) complexes were synthesized and characterized by elemental analysis, one- and two-dimensional NMR spectroscopy, mass spectrometry, and reversed-phase HPLC (log kw) and in one case by X-ray diffraction. Cytotoxicity of the compounds was studied in three human cancer cell lines (CH1, SW480, and A549) by means of the MTT assay, featuring IC50 values to the low micromolar range. Furthermore a selected set of compounds was investigated in additional cancer cell lines (P31 and P31/cis, A2780 and A2780/cis, SW1573, 2R120, and 2R160) with regard to their resistance patterns, offering a distinctly different scheme compared to cisplatin. To gain further insights into the mode of action, drug uptake, DNA synthesis inhibition, cell cycle effects, and induction of apoptosis were determined for two characteristic substances.
U2 - 10.1021/jm301645g
DO - 10.1021/jm301645g
M3 - Article
SN - 0022-2623
VL - 55
SP - 11052
EP - 11061
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 24
ER -
