Bernhardt, Günther and Gust, Ronald and Reile, Herta and vom Orde, Hans Dieter and Müller, Richard and Keller, Christoph and Spruß, Thilo and Schönenberger, Helmut and Burgemeister, Thomas and Mannschreck, Albrecht and Range, Klaus Jürgen and Klement, Ulrich (1992) [1,2-Bis(2-hydroxyphenyl)ethylenediamine]dichloroplatinum(II), a new compound for the therapy of ovarian cancer. III. Detailed evaluation of the antitumor activity of the enantiomeric complexes on the human NIH:OVCAR-3 ovarian cancer cell line. Journal of cancer research and clinical oncology 118 (3), pp. 209-215.
The stereoisomeric [1,2-bis(2-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) complexes were thoroughly tested on the cisplatin-resistant human NIH:OVCAR-3 ovarian cancer cell line. The racemate and its enantiomers produced cytocidal effects at a concentration of 2.5 microM (incubation time 256 h). The meso form, however, was merely cytostatically active. Differences between the enantiomers became evident after a short drug incubation time (1 h) followed by an incubation in drug-free medium (243 h). The S,S-configurated enantiomer (-)-3-PtCl2 proved to be the most active compound. To achieve cytocidal effects concentrations of 2.5-5.0 microM and incubation times of about 3 h were necessary for (-)-3-PtCl2. This compound is also sufficiently stable under test conditions as shown by the preincubation in cell-free medium for 3 h. These results and the augmentation of its antitumor activity by buthionine sulfoximine recommend the further preclinical development of (-)-3-PtCl2 for clinical use.
|Institutions:|| Chemistry and Pharmacy > Institut für Organische Chemie > Retired Professors > Prof.Dr. Mannschreck|
Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||14 Jan 2009 13:33|
|Last Modified:||01 Feb 2012 14:24|