REILE, H and BERNHARDT, G and KOCH, M and SCHONENBERGER, H and HOLLSTEIN, M and LUX, F (1992) CHEMOSENSITIVITY OF HUMAN MCF-7 BREAST-CANCER CELLS TO DIASTEREOISOMERIC DIAQUA(1,2-DIPHENYLETHYLENEDIAMINE) PLATINUM(II) SULFATES AND SPECIFIC PLATINUM ACCUMULATION. CANCER CHEMOTHERAPY AND PHARMACOLOGY, 30 (2). pp. 113-122. ISSN 0344-5704,
Full text not available from this repository.Abstract
Cisplatin, raceme-diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]platinum(II) sulfate (compound I), meso-diaqua[1,2-bis(4-fluorophenyl)ethylenediamine]platinum(II) sulfate (compound II), and meso-diaqua[1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]platinum(II) sulfate (compound III) were compared with regard to their effect on the MCF-7 breast cancer cell line in vitro. At equimolar concentrations (5-mu-M), cisplatin, compound I, and compound II were equiactive after 231 h drug exposure. whereas compound III was ineffective. Although compounds I and II showed markedly greater inactivation than did cisplatin after 6 h incubation with culture medium, compound I (but not compound II) exhibited antitumor activity equivalent to that of cisplatin when cells were exposed to the drugs for 6 h. Platinum measurements by neutron-activation analysis revealed that compound I was selectively and rapidly accumulated by MCF-7 cells, resulting in a high degree of DNA platination within the first few hours of drug exposure. However, when the drug-exposure period was long enough, platinum enrichment was not reflected in an overall difference in the cytotoxicity of compound I vs cisplatin. Nevertheless, compound I should be superior to cisplatin in vivo, provided that effective plasma levels can be maintained for about 6 h.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | INHIBITING <1,2-BIS(FLUOROPHENYL)ETHYLENEDIAMINE>PLATINUM(II) COMPLEXES; ANTI-TUMOR ACTIVITY; RAT-KIDNEY; CIS-DIAMMINEDICHLOROPLATINUM(II); CARCINOMA; TRANSPORT; CISPLATIN; BINDING; AGENTS; LINE; INTRACELLULAR ACCUMULATION; CISPLATINUM ANALOGS; MCF-7 CELLS |
| Depositing User: | Dr. Gernot Deinzer |
| Last Modified: | 19 Oct 2022 08:44 |
| URI: | https://pred.uni-regensburg.de/id/eprint/54506 |
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