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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
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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.
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| Dokumentenart | Artikel | ||||||||||||||||||||
| Titel eines Journals oder einer Zeitschrift | Archiv der Pharmazie | ||||||||||||||||||||
| Band: | 323 | ||||||||||||||||||||
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| Nummer des Zeitschriftenheftes oder des Kapitels: | 3 | ||||||||||||||||||||
| Seitenbereich: | S. 133-140 | ||||||||||||||||||||
| Datum | 1990 | ||||||||||||||||||||
| Institutionen | Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische / Medizinische Chemie II (Prof. Buschauer) | ||||||||||||||||||||
| Identifikationsnummer |
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| Klassifikation |
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| Dewey-Dezimal-Klassifikation | 500 Naturwissenschaften und Mathematik > 570 Biowissenschaften, Biologie 500 Naturwissenschaften und Mathematik > 540 Chemie | ||||||||||||||||||||
| Status | Veröffentlicht | ||||||||||||||||||||
| Begutachtet | Ja, diese Version wurde begutachtet | ||||||||||||||||||||
| An der Universität Regensburg entstanden | Ja | ||||||||||||||||||||
| URN der UB Regensburg | urn:nbn:de:bvb:355-epub-48329 | ||||||||||||||||||||
| Dokumenten-ID | 4832 |
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