| Dokumentenart: | Artikel | ||||||||||||||||||||||||||||
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| Titel eines Journals oder einer Zeitschrift: | Archiv der Pharmazie | ||||||||||||||||||||||||||||
| Verlag: | WILEY-V C H VERLAG GMBH | ||||||||||||||||||||||||||||
| Ort der Veröffentlichung: | WEINHEIM | ||||||||||||||||||||||||||||
| Band: | 337 | ||||||||||||||||||||||||||||
| Nummer des Zeitschriftenheftes oder des Kapitels: | 6 | ||||||||||||||||||||||||||||
| Seitenbereich: | S. 349-359 | ||||||||||||||||||||||||||||
| Datum: | 2004 | ||||||||||||||||||||||||||||
| Institutionen: | Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische / Medizinische Chemie II (Prof. Buschauer) Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische / Medizinische Chemie II (Prof. Buschauer) | ||||||||||||||||||||||||||||
| Sonstige Projekte: | SFB 234 | ||||||||||||||||||||||||||||
| Identifikationsnummer: |
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| Klassifikation: |
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| Stichwörter / Keywords: | DIAQUA(1,2-DIPHENYLETHYLENEDIAMINE) PLATINUM(II) SULFATES; INHIBITING PROPERTIES; ANTICANCER DRUGS; SERUM-ALBUMIN; MAJOR ADDUCT; IN-VITRO; CISPLATIN; DNA; CIS-DIAMMINEDICHLOROPLATINUM(II); CYTOTOXICITY; reactivity; inactivation kinetics; drug accumulation; anti-breast cancer activity | ||||||||||||||||||||||||||||
| Dewey-Dezimal-Klassifikation: | 600 Technik, Medizin, angewandte Wissenschaften > 615 Pharmazie 500 Naturwissenschaften und Mathematik > 540 Chemie 600 Technik, Medizin, angewandte Wissenschaften > 610 Medizin | ||||||||||||||||||||||||||||
| Status: | Veröffentlicht | ||||||||||||||||||||||||||||
| Begutachtet: | Ja, diese Version wurde begutachtet | ||||||||||||||||||||||||||||
| An der Universität Regensburg entstanden: | Ja | ||||||||||||||||||||||||||||
| Dokumenten-ID: | 4835 |
Web of ScienceZusammenfassung
The marked activity of [meso-1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]platinum(II) (meso-3-PtLL', L,L' = Cl-2 or L = OH2, L' = OSO3) on the hormone-sensitive MXT-M-3,2 breast cancer implanted in mice is most probably due to a mechanism based on the reduction of the endogenous estrogen level. Cytotoxic effects which are poorly pronounced in experiments on several breast cancer cell ...
Zusammenfassung
The marked activity of [meso-1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]platinum(II) (meso-3-PtLL', L,L' = Cl-2 or L = OH2, L' = OSO3) on the hormone-sensitive MXT-M-3,2 breast cancer implanted in mice is most probably due to a mechanism based on the reduction of the endogenous estrogen level. Cytotoxic effects which are poorly pronounced in experiments on several breast cancer cell lines (e.g. MCF-7), do not significantly contribute to the anti-breast cancer activity of this compound. In contrast to this, the standard cisplatin and the structurally related comparison compound [meso-1,2-bis(4-fluorophenyl)ethylenediamine]platinum(II) (meso-4-PtLL', L,L' = Cl-2 or L = OH2, L' = OSO3) are strongly active in vivo as well as in vitro. Both effects entail programmed cell death, which is responsible for the inhibition of the tumor growth. The minor cytotoxicity of meso-3-PtLL' in breast cancer cell cultures is caused neither by an inappropriate rate of reaction with bionucleophiles (e.g. by a too fast inactivation by plasma proteins) nor solely by the observed poor absorption by the tumor cells resulting in an insufficient drug concentration at the DNA. Additionally, an impeded reaction with biologically important, guanine-rich sequences of DNA (owing to the 2,6-standing F atoms which hinder the drug-target interaction) must be assumed as cause of its marginal cytotoxicity.
Metadaten zuletzt geändert: 29 Sep 2021 07:28
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