REDUCTION OF THE ESTROGENIC SIDE-EFFECTS OF THE MAMMARY TUMOR-INHIBITING DRUG [1,2-BIS(2,6-DICHLORO-4-HYDROXYPHENYL)-ETHYLENEDIAMINE]DICHLOROPLATINUM(II) BY VARIATION OF RING SUBSTITUENTS

GUST, R and KARL, J and FADERL, M and SCHONENBERGER, H (1995) REDUCTION OF THE ESTROGENIC SIDE-EFFECTS OF THE MAMMARY TUMOR-INHIBITING DRUG [1,2-BIS(2,6-DICHLORO-4-HYDROXYPHENYL)-ETHYLENEDIAMINE]DICHLOROPLATINUM(II) BY VARIATION OF RING SUBSTITUENTS. ARCHIV DER PHARMAZIE, 328 (5). pp. 457-463. ISSN 0365-6233,

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Abstract

[1,2-Bis(4-methoxy /4-hydroxyphenyl)ethylenediamine]dichloroplatinum-(II) complexes with Cl-, CH3-, or OCH3-substituents in the ortho-positions of the aromatic rings (meso-1-PtCl2, D,L-1-PtCl2, meso-2 PtCl2, D,L-2-PtCl2, meso-3-PtCl2, meso-4-PtCl2, meso-5-PtCl2) were tested on the MDA-MB 231 breast cancer cell line, the lymphocytic leukemia P388, and the estrogen receptor-positive and -negative MXT mammary carcinoma of the mouse (MXT,ER(+)-MC, MXT,ER(-)-MC), The comparison of the effects of methoxy-substituted complexes (meso-1-PtCl2, D,L-1-PtCl2, meso-3-PtCl2) with those of the respective hydroxy substituted ones (meso-2-PtCl2, D,L-2-PtCl2, meso-4-PtCl2) shows that a reduction of estrogenic effects as well as a total loss of the mammary tumor-inhibiting activity takes place on methylation of the 4-OH group. The exchange of the 2,6-standing chlorine atoms by methyl groups in meso-2-PtCl2 led to the non-estrogenic, but on the MXT,ER(+)-MC highly effective derivative meso-CPtCl2 which proved to be also cytotoxic on ER(-)-tumors such as MXT,ER(-)-MC, and the P 388 leukemia.

Item Type: Article
Uncontrolled Keywords: PLATINUM COMPLEX; ANTITUMOR;
Depositing User: Dr. Gernot Deinzer
Last Modified: 19 Oct 2022 08:37
URI: https://pred.uni-regensburg.de/id/eprint/52550

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