A novel cytotoxic cerium complex: aquatrichloridobis(1,10-phenanthroline)cerium(III) (KP776). Synthesis, characterization, behavior in H2O, binding towards biomolecules, and antiproliferative activity.
The lanthanide complex aquatrichloridobis(1,10-phenanthroline)cerium(III) [Ce(phen)2(H2O)Cl3] (KP776) was fully characterized by elemental analysis, IR-, and 1H- and 13C-NMR spectroscopy, as well as TG/DTA measurements, and its behavior in H2O, important for the application as a chemotherapeutic, was studied. In addition, the binding of KP776 to nucleotides and single serum proteins was investigated by capillary electrophoresis, whereas binding to proteins in human plasma was observed by ICP-MS. The compound shows promising anticancer properties in vitro: proliferation of human cancer cell lines is strongly inhibited with IC(50) values in the very low micromolar range.
Biba
Florian
F
University of Vienna, Institute of Inorganic Chemistry, Waehringer Strasse 42, A-1090 Vienna.
Groessl
Michael
M
Egger
Alexander
A
Jakupec
Michael A
MA
Keppler
Bernhard K
BK
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001798:Blood Proteins / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D002563:Cerium / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D019075:Electrophoresis, Capillary; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D011485:Protein Binding; D013055:Spectrophotometry, Infrared; D013696:Temperature; D013997:Time Factors; D014867:Water / Q000737:chemistry*
D000970:Antineoplastic Agents; D001798:Blood Proteins; D009942:Organometallic Compounds; C547371:aquatrichloridobis(1,10-phenanthroline)cerium(III); D014867:Water; D002563:Cerium