Chemosensitivity of human MCF-7 breast cancer cells to diastereoisomeric diaqua(1,2-diphenylethylenediamine) platinum(II) sulfates and specific platinum accumulation

URN to cite this document:

urn:nbn:de:bvb:355-epub-48309 Copy

DOI to cite this document:

10.5283/epub.4830 Copy

Reile, Herta ; Bernhardt, Günther ; Koch, Marion ; Schönenberger, Helmut ; Hollstein, Michael ; Lux, Franz

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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:	Cancer chemotherapy and pharmacology
Volume:	30
Number of Issue or Book Chapter:	2
Page Range:	pp. 113-122
Date:	1992
Institutions:	Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:	SFB 234
Identification Number:	Value Type 1600591 PubMed ID
Classification:	Notation Type Breast Neoplasms/drug therapy MESH Cisplatin/pharmacokinetics MESH Culture Media MESH DNA, Neoplasm/metabolism MESH Drug Screening Assays, Antitumor MESH Drug Stability MESH Humans MESH Kinetics MESH Organoplatinum Compounds/pharmacology MESH Platinum/pharmacokinetics MESH Stereoisomerism MESH Time Factors MESH Tumor Cells, Cultured/drug effects MESH
Dewey Decimal Classification:	500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences
Status:	Published
Refereed:	Yes, this version has been refereed
Created at the University of Regensburg:	Partially
Item ID:	4830

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Abstract

Cisplatin, raceme-diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]platinu m(II) sulfate (compound I), meso-diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]-platinum(II) sulfate (compound II), and meso-diaqua[1,2-bis(2,6-dichloro-4- hydroxyphenyl)ethylenediamine]platinum(II) sulfate (compound III) were compared with regard to their effect on the MCF-7 breast cancer cell line in vitro. At equimolar ...

Abstract

Cisplatin, raceme-diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]platinu m(II) sulfate (compound I), meso-diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]-platinum(II) sulfate (compound II), and meso-diaqua[1,2-bis(2,6-dichloro-4- hydroxyphenyl)ethylenediamine]platinum(II) sulfate (compound III) were compared with regard to their effect on the MCF-7 breast cancer cell line in vitro. At equimolar concentrations (5 microM), cisplatin, compound I, and compound II were equiactive after 231 h drug exposure, whereas compound III was ineffective. Although compounds I and II showed markedly greater inactivation than did cisplatin after 6 h incubation with culture medium, compound I (but not compound II) exhibited antitumor activity equivalent to that of cisplatin when cells were exposed to the drugs for 6 h. Platinum measurements by neutron-activation analysis revealed that compound I was selectively and rapidly accumulated by MCF-7 cells, resulting in a high degree of DNA platination within the first few hours of drug exposure. However, when the drug-exposure period was long enough, platinum enrichment was not reflected in an overall difference in the cytotoxicity of compound I vs cisplatin. Nevertheless, compound I should be superior to cisplatin in vivo, provided that effective plasma levels can be maintained for about 6 h.

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