title: Bis- and Tetrakis(carboxylato)platinum(IV) complexes with mixed axial ligands - synthesis, characterization, and cytotoxicity.
abstract: A series of twelve novel diamminetetrakis(carboxylato)platinum(IV) and 18 novel bis(carboxylato)dichlorido(ethane-1,2-diamine)platinum(IV) complexes with mixed axial carboxylato ligands was synthesized and characterized by multinuclear (1) H-, (13) C-, (15) N-, and (195) Pt-NMR spectroscopy. Their cytotoxic potential was evaluated (by MTT assay) against three human cancer cell lines derived from ovarian teratocarcinoma (CH1/PA-1), lung (A549), and colon carcinoma (SW480). In the cisplatin-sensitive CH1/PA-1 cancer cell line, diamminetetrakis(carboxylato)platinum(IV) complexes showed IC50 values in the low micromolar range, whereas, for the most lipophilic compounds of the bis(carboxylato)dichlorido(ethane-1,2-diamine)platinum(IV) series, IC50 values in the nanomolar range were found.
authors: Institute of Inorganic Chemistry, University of Vienna, Waehringer Strasse 42, AT-1090 Vienna (phone: +43-1-427752600; fax: +43-1-427752680).
authors: Björn R
authors: BR
authors: Hoffmeister
authors: Michaela
authors: M
authors: Hejl
authors: Mahsa S
authors: MS
authors: Adib-Razavi
authors: Michael A
authors: MA
authors: Jakupec
authors: Markus
authors: M
authors: Galanski
authors: Bernhard K
authors: BK
authors: Keppler
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D002945:Cisplatin / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D008024:Ligands; D009944:Organoplatinum Compounds; D002945:Cisplatin
keywords: 195Pt-NMR Spectroscopy; Cytotoxic activity; Platinum complexes