| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Journal of Cancer Research and Clinical Oncology | ||||
| Volume: | 124 | ||||
| Number of Issue or Book Chapter: | 11 | ||||
| Page Range: | pp. 585-597 | ||||
| Date: | 1998 | ||||
| Additional Information (public): | CAN 130:90198 1-6 Pharmacology 184895-28-1P; 185069-09-4P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses) ([rac-1,2-bis(4-fluorophenyl)ethylenediamine][cyclobutane-1,1-dicarboxylato]platinum(II), a novel, highly active carboplatin deriv., antitumor effect); 5445-51-2 (1,1-Cyclobutanedicarboxylic acid); 184895-34-9; 185069-15-2 Role: RCT (Reactant), RACT (Reactant or reagent) ([rac-1,2-bis(4-fluorophenyl)ethylenediamine][cyclobutane-1,1-dicarboxylato]platinum(II), a novel, highly active carboplatin deriv., synthesis) | ||||
| 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) | ||||
| Identification Number: |
| ||||
| Keywords: | Antitumor agents ([rac-1,2-bis(4-fluorophenyl)ethylenediamine][cyclobutane-1,1-dicarboxylato]platinum(II), a novel, highly active carboplatin deriv., antitumor effect); Molecular structure ([rac-1,2-bis(4-fluorophenyl)ethylenediamine][cyclobutane-1,1-dicarboxylato]platinum(II), a novel, highly active carboplatin deriv., mol. structure); fluorophenyl ethylendiamine cyclobutane carboxylatoplatinum synthesis anticancer; carboplatin deriv anticancer | ||||
| Dewey Decimal Classification: | 500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 5478 |
Abstract
The synthesis of the diastereomeric [1,2-bis(4-fluorophenyl)ethylendiamine][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 physiol. environment were described (ref. complexes: the dichloro- and sulfatoplatinum(II) analogs, carboplatin and cisplatin). Rac-4F-Pt(CBDC) ...

Abstract
The synthesis of the diastereomeric [1,2-bis(4-fluorophenyl)ethylendiamine][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 physiol. environment were described (ref. complexes: the dichloro- and sulfatoplatinum(II) analogs, carboplatin and cisplatin). Rac-4F-Pt(CBDC) equaled cisplatin and surpassed carboplatin in its effect on human breast cancer cell lines (MCF-7 and MDA-MB-231). Rac-4F-Pt(CBDC) was largely insensitive against attack of nucleophiles (Cl-). In vitro studies on the binding of rac-4F-Pt(CBDC) to albumin showed that the non-protein-bound fraction was comparable to that of carboplatin. The distinctly better anti-breast cancer activity of rac-4F-Pt(CBDC) than of carboplatin was attributed to its ability to accumulate in the tumor cells. The human ovarian cancer cell line NIH-OVCAR-3 was also strongly inhibited by rac-4F-Pt(CBDC).
Metadata last modified: 24 May 2018 10:11
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