| Item type: | Article | ||||||||||||||||||||||||||||
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| Journal or Publication Title: | Archiv der Pharmazie | ||||||||||||||||||||||||||||
| Publisher: | WILEY-V C H VERLAG GMBH | ||||||||||||||||||||||||||||
| Place of Publication: | WEINHEIM | ||||||||||||||||||||||||||||
| Volume: | 337 | ||||||||||||||||||||||||||||
| Number of Issue or Book Chapter: | 6 | ||||||||||||||||||||||||||||
| Page Range: | pp. 349-359 | ||||||||||||||||||||||||||||
| Date: | 2004 | ||||||||||||||||||||||||||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) | ||||||||||||||||||||||||||||
| Projects (Historical): | SFB 234 | ||||||||||||||||||||||||||||
| Identification Number: |
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| Classification: |
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| 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 Decimal Classification: | 600 Technology > 615 Pharmacy 500 Science > 540 Chemistry & allied sciences 600 Technology > 610 Medical sciences Medicine | ||||||||||||||||||||||||||||
| Status: | Published | ||||||||||||||||||||||||||||
| Refereed: | Yes, this version has been refereed | ||||||||||||||||||||||||||||
| Created at the University of Regensburg: | Yes | ||||||||||||||||||||||||||||
| Item ID: | 4835 |
Web of ScienceAbstract
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 ...
Abstract
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.
Metadata last modified: 29 Sep 2021 07:28
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