Journal ArticleDOI
The tumor-inhibiting effect of isomeric dichloro(diphenylethylenediamine)platinum(II) complexes.
Beate Wappes,Margaretha Jennerwein,Erwin von Angerer,J. Engel,Helmut Schönenberger,Henri Brunner,M. Schmidt,Mathias Berger,D. Schmäh,Siegfried Seeber +9 more
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TLDR
The differences in activity of the diastereomers (±)-2d and meso-2d, for which distinct influences on the DNA secondary structure can be demonstrated CD spectroscopically may be explained by a steric hindrance of the drug-DNA interaction.Abstract:
Ring unsubstituted dichloro(diphenylethylenediamine)platinum(II) complexes show a dependence of their antitumor activity on the configuration and position of phenyl rings in ethylenediamine ligand. Dichloro(1,1-diphenylethylenediamine)platinum(II) (1d) and meso-dichloro(1,2-diphenylethylenediamine)-platinum(II) (meso-2d) have a weaker effect on the human breast-cancer cell line MDA-MB 231 and on rat leukemia L5222 than (±)-dichloro(1,2-diphenylethylenediamine)platinum(II) ((+)-2d) and its enantiomers (+)-2d and (-)-2d which cause marked and comparable inhibition of both tumors; (±)-2d is also active on ADJ/PC 6 plasmacytoma of the mouse and on cisplatin-, daunomycin-, and cisplatin/daunomycin-resistant Ehrlich ascites tumors of the mouse. The differences in activity of the diastereomers (±)-2d and meso-2d, for which distinct influences on the DNA secondary structure can be demonstrated CD spectroscopically may be explained by a steric hindrance of the drug-DNA interaction.read more
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In vitro antitumour activity of two isomeric cyclopalladiated compounds derived from benzoylbenzylidenimines
TL;DR: The DNA thermal stabilizing effect and antitumour properties of two diastereoisomeric cyclopalladiated compounds derived from benzoylbenzylideneimines have been studied in this paper.
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Chemosensitivity of human MCF-7 breast cancer cells to diastereoisomeric diaqua(1,2-diphenylethylenediamine) platinum(II) sulfates and specific platinum accumulation.
TL;DR: 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, which should be superior to cisplatin in vivo.
Journal ArticleDOI
Antitumor complexes of platinum with carrier molecules. 2 [1]. Mixed complexes of amino acids and tert-butylamine
Erik Bersanetti,Alessandro Pasini,Gabriella Pezzoni,Graziella Pratesi,Guiseppina Savi,Rossana Supino,Franco Zunino +6 more
TL;DR: In this paper, two inert ligands bound to platinum in the cis-position were synthesized with the aim of obtaining liposoluble cisplatin analogues bound to natural carrier groups.
Journal ArticleDOI
Influence of ring substituents on the antitumor effect of dichloro(1,2-diphenylethylenediamine)platinum(II) complexes
Margaretha Jennerwein,Beate Wappes,Ronald Gust,Helmut Schönenberger,J. Engel,Siegfried Seeber,R. Osieka +6 more
TL;DR: Diastereomeric para-substituted dichloro-(1,2-diphenylethylenediamine)platinum(II) complexes were synthesized and tested for their antitumor activity on the human MDA-MB 231 breast cancer cell line and the P 388 leukemia of the mouse.
Journal ArticleDOI
Neue Cisplatin-Analoga — auf dem Weg zu besseren Cancerostatica
Alessandro Pasini,Franco Zunino +1 more
TL;DR: In this article, the authors discuss the erhohte Wirkstoffkonzentration im Tumorgewebe zu erreichen sein, nach einer kurzen Betrachtung der „traditionellen” Analoga, die unseres Erachtens erfolgversprechendest Wege zu neuartigen Cisplatin-Analoga diskutieren.
References
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Platinum Compounds: a New Class of Potent Antitumour Agents
TL;DR: The platinum compounds inhibit sarcoma 180 and leukaemia L1210 in mice and reversibly inhibit cell division in Gram-negative rods1–4.
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Binding of cis- and trans-dichlorodiammineplatinum(II) to DNA: evidence for unwinding and shortening of the double helix
TL;DR: The antitumor drug cis-dichlorodiammineplatinum(II) (cis-DDP) and the inactive trans isomer bind and produce cooperative changes in closed and nicked circular duplex DNA's to alter the degree of supercoiling.
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Anti-tumour platinum complexes : relationships between chemical properties and activity
TL;DR: In this article, the authors present a range of amine complexes of the type [Pt A S X 2] (A z = two monoden-to-one or one-identare amine ]-interfaces.
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Modifications of the DNA secondary structure upon platinum binding: a proposed model
TL;DR: Spectrofluorometry, ultraviolet spectroscopy, circular dichroism, melting curves, kinetics and electron microscopy were found powerful in the differentiation of the DNA secondary structure modifications upon platinum binding.