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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Inorganica Chimica Acta | ||||
| Volume: | 357 | ||||
| Number of Issue or Book Chapter: | 15 | ||||
| Page Range: | pp. 4452-4466 | ||||
| Date: | 2004 | ||||
| Additional Information (public): | CAN 142:126560 1-3 Pharmacology 792912-73-3P; 792912-74-4P; 792912-75-5P; 792912-77-7P; 827325-34-8P; 827325-35-9P; 827325-36-0P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses) (carboplatin derivs. with superior antitumor activity compared to the parent compd.); 99038-34-3 Role: PAC (Pharmacological activity), THU (Therapeutic use), BIOL (Biological study), USES (Uses) (carboplatin derivs. with superior antitumor activity compared to the parent compd.); 5445-51-2 (1,1-Cyclobutanedicarboxylic acid); 15663-27-1 (Cisplatin); 38780-40-4; 41575-94-4; 52241-26-6; 99173-61-2; 123812-76-0; 123812-77-1; 161096-40-8; 792912-76-6 Role: RCT (Reactant), RACT (Reactant or reagent) (carboplatin derivs. with superior antitumor activity compared to the parent compd.); 35995-55-2P; 51816-01-4P (1,1-Cyclobutanedicarbonyl dichloride); 54166-15-3P; 89582-02-5P; 89639-43-0P; 99974-66-0P; 825620-41-5P; 827032-76-8P; 827032-77-9P; 827032-78-0P; 827032-79-1P; 827032-80-4P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (carboplatin derivs. with superior antitumor activity compared to the parent compd.) | ||||
| Institutions: | Chemistry and Pharmacy > Institut für Anorganische Chemie Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) | ||||
| Identification Number: |
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| Keywords: | Antitumor agents; Bladder; Human; Structure-activity relationship (carboplatin derivs. with superior antitumor activity compared to the parent compd.); Ovary, neoplasm (cisplatin-resistant, carboplatin derivs. with superior antitumor activity compared to the parent compd.); carboplatin deriv prepn | ||||
| 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: | 5472 |
Abstract
A series of new carboplatin derivs. 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, resp., as non-leaving groups. The antiproliferative activity of the new carboplatin analogs differing ...
Abstract
A series of new carboplatin derivs. 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, resp., as non-leaving groups. The antiproliferative activity of the new carboplatin analogs differing in the cyclobutanedicarboxylato 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 compds. were the 3-fluoro, 3-chloro and 3,3-difluoro derivs. 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.
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