[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

URN to cite this document:

urn:nbn:de:bvb:355-epub-48137 Copy

DOI to cite this document:

10.5283/epub.4813 Copy

Bernhardt, Günther ; Gust, Ronald ; Reile, Herta ; vom Orde, Hans Dieter ; Müller, Richard ; Keller, Christoph ; Spruß, Thilo ; Schönenberger, Helmut ; Burgemeister, Thomas ; Mannschreck, Albrecht ; Range, Klaus Jürgen ; Klement, Ulrich

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Date of publication of this fulltext: 05 Aug 2009 13:48

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Details

Item type:	Article
Journal or Publication Title:	Journal of cancer research and clinical oncology
Publisher:	Springer
Volume:	118
Number of Issue or Book Chapter:	3
Page Range:	pp. 209-215
Date:	1992
Institutions:	Chemistry and Pharmacy > Institut für Organische Chemie > Alumni or Retired Professors > Prof.Dr. Mannschreck Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Identification Number:	Value Type 1548286 PubMed ID
Classification:	Notation Type Antineoplastic Agents/pharmacology MESH Buthionine Sulfoximine MESH Cell Line MESH Cisplatin/pharmacology MESH Female MESH Glutathione/metabolism MESH Humans MESH Methionine Sulfoximine/analogs & derivatives MESH Organoplatinum Compounds/pharmacology MESH Ovarian Neoplasms/drug therapy MESH Stereoisomerism MESH Structure-Activity Relationship MESH Tumor Cells, Cultured/drug effects MESH
Dewey Decimal Classification:	500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences 600 Technology > 610 Medical sciences Medicine
Status:	Published
Refereed:	Yes, this version has been refereed
Created at the University of Regensburg:	Yes
Item ID:	4813

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Abstract

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 ...

Abstract

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.

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