| 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. 335-348 | ||||||||||||||||||||||||||||||||||
| Date: | 2004 | ||||||||||||||||||||||||||||||||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy 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: | TUMOR INHIBITING PROPERTIES; IMMUNE-RESPONSE MODIFIER; PROGRAMMED CELL-DEATH; MOUSE MAMMARY-TUMOR; VARIABLE SUBSTITUENTS; 2-PHENYL RING; <1,2-BIS(2,6-DIHALO-3-HYDROXYPHENYL)ETHYLENEDIAMINE>PLATINUM(II) COMPLEXES; CYCLE ARREST; DNA-REPAIR; CISPLATIN; [1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]platinum(II) complexes; anti-breast cancer activity; mode of action | ||||||||||||||||||||||||||||||||||
| Dewey Decimal Classification: | 600 Technology > 615 Pharmacy 500 Science > 540 Chemistry & allied sciences | ||||||||||||||||||||||||||||||||||
| Status: | Published | ||||||||||||||||||||||||||||||||||
| Refereed: | Yes, this version has been refereed | ||||||||||||||||||||||||||||||||||
| Created at the University of Regensburg: | Yes | ||||||||||||||||||||||||||||||||||
| Item ID: | 4836 |
Web of ScienceAbstract
Aqua[meso-1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]sulfato-platinum(II) (meso-3-PtSO4) and its racemate (rac-3-PtSO4) are highly active on the hormone-sensitive MXT-M-3,2 breast cancer of the mouse. In vitro, on the MXT+ cell culture derived from this tumor, however, they are inactive (meso-3PtSO(4)) or moderately active (rac-3-PtSO4) in concentrations corresponding to levels of these ...
Abstract
Aqua[meso-1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]sulfato-platinum(II) (meso-3-PtSO4) and its racemate (rac-3-PtSO4) are highly active on the hormone-sensitive MXT-M-3,2 breast cancer of the mouse. In vitro, on the MXT+ cell culture derived from this tumor, however, they are inactive (meso-3PtSO(4)) or moderately active (rac-3-PtSO4) in concentrations corresponding to levels of these drugs in animal experiments. The in vivo effect is mainly caused by a reduction of the endogenous estrogen level in the host animals due to an interference with the ovarian steroid biosynthesis as demonstrated for meso-3PtSO(4). Therefore, a reversal of the breast cancer inhibiting effect of meso-3PtSO(4) can be achieved by simultaneous estrone administration. Histological results on ovaries, uterus, and tumor of meso-3-PtSO4-treated mice also favor such a mode of action. However, especially for rac-3-PtSO4 cytotoxic effects contributing to the anti-breast cancer activity cannot be excluded. Considerations on the mode of action of Pt-bomplexes which inhibit breast cancer by interference with estrogen receptor mediated processes of growth control and with DNA replication are presented.
Metadata last modified: 29 Sep 2021 07:28
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