Gust, Ronald and Krauser, Rudolf and Schmid, Beate and Schönenberger, Helmut (1998) Synthesis and antitumor activity of [1,2-bis(4-fluorophenyl)ethylenediamine][dicarboxylato]platinum(II) complexes. ARCHIV DER PHARMAZIE, 331 (1). pp. 27-35. ISSN 0365-6233, 1521-4184
Full text not available from this repository.Abstract
The synthesis of the diastereomeric [1,2-bis(4-fluorophenyl)ethylenediamine][dicarboxylato]platinum(II) complexes, rac- and meso-4F-Pt(X) [X: oxalato (Ox), malonato (Mal), hydroxymalonato (OHMal), phenylmalonato (PhMal), tetrahydro-4H-pyran-4,4-dicarboxylato (Thpdc)], the evaluation of their structure, water solubility, resistance against attack by nucleophiles, and, growth inhibiting properties on the human MCF-7 breast cancer cell line are described [parent compounds: rac-4F-Pt(CBDC) and meso-4F-Pt(CBDC); reference complexes: carboplatin, cisplatin, rac- and meso-4F-PtCl2]. The most active 4F-Pt(X) complexes, rac-4F-Pt(Mal), rac-4F-Pt(OHMal) and rac-4F-Pt(Thpdc), equal the parent compound rac-4F-Pt(CBDC) as well as cisplatin and surpass carboplatin in their effect on the MCF-7 breast cancer cell line. Their water solubility, which is of importance for an application in the cancer chemotherapy, is higher than that of rac-4F-Pt(CBDC), especially in the case of rac-4F-Pt(OHMal) and rac-4F-Pt(Thpdc). In comparison to the dichloro-platinum(II) analogue (4F-PtCl2) the stability of the three compounds in the presence of the strong nucleophile iodide is markedly enhanced, which means a reduction of the protein bound drug fraction in the blood and tissue compartments accompanied by an increase of the active, free drug level. The found physiochemical properties of these compounds meet the requirements for the transferability of their promising breast cancer inhibiting effects detected in cell culture experiments to in vivo conditions.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CHEMOSENSITIVITY; PLATINUM(II); CELLS; synthesis; water solubility; stability; antitumor activity; human MCF-7 breast cancer cell line |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 28 Mar 2023 04:46 |
| Last Modified: | 28 Mar 2023 04:46 |
| URI: | https://pred.uni-regensburg.de/id/eprint/50165 |
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