Direkt zum Inhalt

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

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

Reile, Herta, Müller, Richard, Gust, Ronald, Laske, Reiner, Krischke, Walter, Bernhardt, Günther, Spruss, Thilo, Jennerwein, Margaretha, Engel, Jürgen und Seeber, Siegfried (1990) 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. Archiv der Pharmazie 323 (3), S. 133-140.

Veröffentlichungsdatum dieses Volltextes: 05 Aug 2009 13:48
Artikel
DOI zum Zitieren dieses Dokuments: 10.5283/epub.4832


Zusammenfassung

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 ...

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.



Beteiligte Einrichtungen


Details

DokumentenartArtikel
Titel eines Journals oder einer ZeitschriftArchiv der Pharmazie
Band:323
Nummer des Zeitschriftenheftes oder des Kapitels:3
Seitenbereich:S. 133-140
Datum1990
InstitutionenChemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische / Medizinische Chemie II (Prof. Buschauer)
Identifikationsnummer
WertTyp
2344259PubMed-ID
Klassifikation
NotationArt
AnimalsMESH
Antineoplastic Agents/pharmacologyMESH
Cell Survival/drug effectsMESH
Cisplatin/pharmacologyMESH
Leukemia P388/pathologyMESH
Leukemia, Experimental/pathologyMESH
MiceMESH
Organoplatinum Compounds/pharmacologyMESH
Tumor Cells, Cultured/drug effectsMESH
Dewey-Dezimal-Klassifikation500 Naturwissenschaften und Mathematik > 570 Biowissenschaften, Biologie
500 Naturwissenschaften und Mathematik > 540 Chemie
StatusVeröffentlicht
BegutachtetJa, diese Version wurde begutachtet
An der Universität Regensburg entstandenJa
URN der UB Regensburgurn:nbn:de:bvb:355-epub-48329
Dokumenten-ID4832

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