Bernhardt, Guenther and Brunner, Henri and Gruber, Nick and Lottner, Christian and Pushpan, Simi K. and Tsuno, Takashi and Zabel, Manfred (2004) Carboplatin derivatives with superior antitumor activity compared to the parent compound. INORGANICA CHIMICA ACTA, 357 (15). pp. 4452-4466. ISSN 0020-1693, 1873-3255
Full text not available from this repository. (Request a copy)Abstract
A series of new carboplatin derivatives was synthesized by introducing fluoro, chloro, bromo and hydroxy substituents into the cyclobutane ring. The carboxylic acid groups were used for the complexation with platinum(II) fragments bearing two ammonia and (RR/SS)-trans-1,2-diaminocyclohexane ligands, respectively, as non-leaving groups. The antiproliferative activity of the new carboplatin analogues differing in the cyclobutanedicarboxylate ligands and the type of platinum fragment were studied in tests with J82 bladder cancer cells and SK-OV-3 as well as cisplatin-resistant NIH:OVCAR-3 ovarian cancer cells. The most active compounds were the 3-fluoro, 3-chloro and 3,3-difluoro derivatives of carboplatin. NMR spectroscopy showed that cis-diammine(3-chloro-1,1-cyclobutanedicarboxylato)platinum(II) was hydrolyzed much faster than carboplatin explaining its higher cytostatic activity. (C) 2004 Elsevier B.V. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | SPECTRUM DEOXOFLUORINATING AGENT; ENHANCED THERMAL-STABILITY; CELL-LINES; BIS(2-METHOXYETHYL)AMINOSULFUR TRIFLUORIDE; OVARIAN-CANCER; COMPLEXES; THERAPY; ACIDS; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institut für Anorganische Chemie > Alumni or Retired Professors > Prof. Dr. Henri Brunner |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 21 Jun 2021 09:55 |
| Last Modified: | 21 Jun 2021 09:55 |
| URI: | https://pred.uni-regensburg.de/id/eprint/36900 |
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