Tumor inhibiting [1,2-bis(fluorophenyl)ethylenediamine]platinum(II) complexes. Part II: Biological evaluation-in vitro studies on the P 388 D1 leukemia cell line

URN to cite this document:

urn:nbn:de:bvb:355-epub-48329 Copy

DOI to cite this document:

10.5283/epub.4832 Copy

Reile, Herta ; Müller, Richard ; Gust, Ronald ; Laske, Reiner ; Krischke, Walter ; Bernhardt, Günther ; Spruss, Thilo ; Jennerwein, Margaretha ; Engel, Jürgen ; Seeber, Siegfried

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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:	Archiv der Pharmazie
Volume:	323
Number of Issue or Book Chapter:	3
Page Range:	pp. 133-140
Date:	1990
Institutions:	Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Identification Number:	Value Type 2344259 PubMed ID
Classification:	Notation Type Animals MESH Antineoplastic Agents/pharmacology MESH Cell Survival/drug effects MESH Cisplatin/pharmacology MESH Leukemia P388/pathology MESH Leukemia, Experimental/pathology MESH Mice MESH Organoplatinum Compounds/pharmacology 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:	Yes
Item ID:	4832

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Abstract

Experiments on the P 388 D1 cell line (48 h exposure) demonstrate that [1,2-bis-(fluorophenyl)ethylenediamine]platinum(II) complexes are comparably active on the cell number and 3H-thymidine incorporation, irrespective of the position of the fluorine atom (ortho, meta, or para) and the nature of the "leaving group" (Cl- or H2O). However, the compounds of the R,R/S,S series are more active than ...

Abstract

Experiments on the P 388 D1 cell line (48 h exposure) demonstrate that [1,2-bis-(fluorophenyl)ethylenediamine]platinum(II) complexes are comparably active on the cell number and 3H-thymidine incorporation, irrespective of the position of the fluorine atom (ortho, meta, or para) and the nature of the "leaving group" (Cl- or H2O). However, the compounds of the R,R/S,S series are more active than those of the R,S series and comparable to cisplatin. In the "tumor colony forming assay" the R,R/S,S configurated compounds are about ten times as active as cisplatin. The R,R/S,S configurated diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]platinum(II) salts reach their half maximum effect more readily (t1/2 approximately equal to 1.6 h) than their R,S configurated analogues (t1/2 approximately equal to 20 h). A time limited contact of the cells with R,R/S,S configurated diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]platinum(II) salts (-1h) leads to a similar inhibition like a permanent drug exposure indicating a fast uptake of the complex by the tumor cell. In experiments on the Ehrlich ascites tumor of the mouse and on the L 1210 leukemia cell line R,R/S,S-[1,2-bis(4-fluorophenyl)ethylenediamine]dichloroplatinum(II) turns out to be equipotent with cisplatin.

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