[Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in the 2-phenyl ring 3. Investigation of breast cancer inhibiting properties

Gust, Ronald, Faderl, Michael and Schönenberger, Helmut (2000) [Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in the 2-phenyl ring 3. Investigation of breast cancer inhibiting properties. Journal of cancer research and clinical oncology 126 (11), pp. 647-654.

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Abstract

Abstract

In the search for new anti-breast cancer compds. a series of diastereomeric aqua[1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine]sulfatoplatinum(II) complexes was tested on the hormone-sensitive MXT-M-3.2 breast cancer of the mouse. By simultaneous detn. of tumor and uterine wts. at the end of the expt. the authors obtained an insight into the mode of action. Changes in the uterine wts. indicate whether the anti-breast cancer effect of the test substance is caused either by its capability to reduce the endogenous estrogen level via inhibition of estrogen biosynthesis (mechanism B), or by its estrogenic side effects which enhance the immune defense in the host animals (mechanism C). Studies on the [3H]thymidine incorporation into DNA of MDA-MB-231 breast cancer cells showed that all test compds. inhibit DNA synthesis, like cisplatin (mechanism A). However, in comparison to the std. cisplatin, their activities were low. The three most effective test compds. threo-2-PtSO4 (2-phenyl-residue), threo-5-PtSO4 (2-(4-hydroxyphenyl)-residue), and threo-8-PtSO4 (2-(2-fluoro-4-hydroxyphenyl)-residue) seem to exert their anti-breast cancer effect by mechanism B. Moreover, threo-5-PtSO4 was moderately active on the hormone- insensitive MXT-M-3.2 (Ovex) breast cancer of the mouse. Aqua[erythro-1-(2,6-dichloro-4-hydroxyphenyl)-2-(2-chloro-4-hydroxyphenyl) ethylenediamine]sulfato-platinum(II) (erythro-9-PtSO4) was the only breast cancer inhibiting compd. of the series acting mainly according to mechanism C. A minor contribution of mechanism A, impairment of the DNA function in the tumor cell, to the anti-breast cancer activity of these aqua[1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine]sulfatoplatinum(II) complexes cannot be excluded, since such effects are apparent in the MDA-MB-231 as well as in the MCF-7 breast cancer cell line at higher drug concns. In this test series which was performed with the crystal violet chemosensitivity assay, the MCF-7 cells proved to be somewhat more sensitive.

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Item type:

Article

Date:

2000

Additional Information (public):

CAN 135:40383 1-3 Pharmacology 126735-37-3; 128413-06-9; 128413-07-0; 128413-08-1; 128413-09-2; 128413-10-5; 128413-11-6; 128413-12-7; 128413-13-8; 128524-07-2; 128524-08-3; 128524-09-4; 128524-10-7; 128524-11-8; 128524-12-9; 128524-13-0; 128524-14-1 Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), PRP (Properties), THU (Therapeutic use), BIOL (Biological study), USES (Uses) ([Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in 2-Ph ring 3. Investigation of breast cancer inhibiting properties)

Institutions:

Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)

Projects:

SFB 234

Identification Number:

Value	Type
2000:710098	Other

Keywords:

DNA formation ([Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in 2-Ph ring 3. Investigation of breast cancer inhibiting properties) Estrogens Role: BAC (Biological activity or effector, except adverse), BPR (Biological process), BSU (Biological study, unclassified), MFM (Metabolic formation), BIOL (Biological study), FORM (Formation, nonpreparative), PROC (Process) ([Aqua-1-(2,6-dic Structure-activity relationship (antitumor [Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in 2-Ph ring 3. Investigation of breast cancer inhibiting properties) Antitumor agents (mammary gland [Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in 2-Ph ring 3. Investigation of breast cancer inhibiting properties) Mammary gland (neoplasm, inhibitors [Aqua-1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine] sulfatoplatinum(II) complexes with variable substituents in 2-Ph ring 3. Investigation of breast cancer inhibiting properties) antitumor breast phenylethylenediamine platinum complex

Dewey Decimal Classification:

500 Science > 540 Chemistry & allied sciences

Status:

Published

Refereed:

Yes, this version has been refereed

Created at the University of Regensburg:

Yes

Item ID:

17720

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