Schertl, Sabine and Hartmann, Rolf W. and Batzl-Hartmann, Christine and Bernhardt, Guenther and Spruss, Thilo and Beckenlehner, Karin and Koch, Marion and Krauser, Rudolf and Schlemmer, Richard and Gust, Ronald and Schoenberger, Helmut (2004) [1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]platinum(II) complexes, compounds for the endocrine therapy of breast cancer - Mode of action I: Antitumor activity due to the reduction of the endogenous estrogen level. ARCHIV DER PHARMAZIE, 337 (6). pp. 335-348. ISSN 0365-6233, 1521-4184
Full text not available from this repository. (Request a copy)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.
| Item Type: | Article |
|---|---|
| Uncontrolled 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 |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 13 Jul 2021 12:55 |
| Last Modified: | 13 Jul 2021 12:55 |
| URI: | https://pred.uni-regensburg.de/id/eprint/37554 |
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