Gust, Ronald and Schnurr, Beate and Krauser, Rudolf and Bernhardt, Guenther and Koch, Marion and Schmid, Beate and Hummel, Evelyn and Schoenenberger, Helmut (1998) Stability and cellular studies of [rac-1,2-bis(4-f luorophenyl)-ethylenediamine][cyclobutane-1,1-dicarboxylato]platinum(II), a novel, highly active carboplatin derivative. JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY, 124 (11). pp. 585-597. ISSN 0171-5216,
Full text not available from this repository.Abstract
The synthesis of the diastereomeric [1, 2-bis(4-fluorophenyl)ethylenediamine][cyclobutane-1, 1-dicarboxylato]platinum(II) complexes, rac- and meso-4F-Pt(CBDC), the evaluation of their structures, their tumor-inhibiting properties and their stability in physiological environment are described (reference complexes: the dichloro- and sulfatoplatinum(II) analogues, carboplatin and cisplatin). The most interesting diastereomer, rac-4F-Pt(CBDC), equals cisplatin and surpasses carboplatin in its effect on human breast cancer cell lines (MCF-7 and MDA-MB-231). Rac-4F-Pt(CBDC) is largely insensitive against attack of nucleophiles e.g. Cl-, a prerequisite for sufficient stability in vivo and for fewer side effects. In accordance with this, in vitro studies on the binding of rac-4F-Pt(CBDC) to albumin, the main plasma protein, show that the free, non-protein-bound fraction is relatively high, coming close to that of carboplatin. These properties are of importance for the transferability of the promising effects found in the cell culture experiments to in vivo conditions. The distinctly better anti-breast cancer activity of rac-4F-Pt(CBDC) than of carboplatin has been attributed to its ability to accumulate in the tumor cells. The human ovarian cancer cell line NIH-OVCAR-3 is also strongly inhibited by rac-4F-Pt(CBDC).
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ANTITUMOR-ACTIVITY; COMPLEXES; PLATINUM; CANCER; CHEMOSENSITIVITY; CHEMOTHERAPY; CISPLATIN; ALBUMIN; TRIAL; CELLS; synthesis; reactivity; stability; accumulation; breast and ovarian cancer cell lines |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 29 Mar 2023 05:07 |
| Last Modified: | 29 Mar 2023 05:07 |
| URI: | https://pred.uni-regensburg.de/id/eprint/49389 |
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