KRITZENBERGER, J and BERNHARDT, G and GUST, R and PISTOR, P and SCHONENBERGER, H and YERSIN, H (1993) DICHLOROBIS(CYCLOALKYLAMINE)PLATINUM(II) COMPLEXES STRUCTURE-ACTIVITY RELATIONSHIP ON THE HUMAN MDA-MB-231 BREAST-CANCER CELL-LINE. MONATSHEFTE FUR CHEMIE, 124 (5). pp. 587-604. ISSN 0026-9247,
Full text not available from this repository.Abstract
The syntheses of dichlorobis(cycloalkylamine)platinum(II) complexes with cis and trans cycloalkylamine ligands [cis-PtCl2(C3H5NH2)2 to cis-PtCl2(C8H15NH2)2 (3-8) and trans-PtCl2-(C7H13NH2)2 (9) and trans-PtCl2(C8H15NH2)2 (10)] are described. The distinction between cis and trans isomers was achieved by H-1-NMR spectroscopy. The antitumor activity was determined on the cell proliferation of the human MDA-MB-231 breast cancer cell line during long-term drug exposure. The complexes with small cycloalkylamine ligands (3-6) were inferior, those with large cycloalkylamine ligands were comparable (7) or superior (8) to cisplatin. Surprisingly, the cis/trans isomers 7/9 and 8/10 were equally active. All cycloalkylamine ligands were inactive. IR-spectroscopic studies showed that the size of the cycloalkylamine ring does not lead to significant differences in the Pt-Cl binding strength. Therefore it is assumed that the markedly stronger antitumor activity of the higher homologues, 7-10, is not the result of a faster reaction with bionucleophils such as DNA. A possible explanation of the high activity of 7-10 is the strong lipophilicity of the complexes. This assumption was confirmed by toxicity tests against confluent cultures.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DNA-POLYMERASE-I; PLATINUM COMPLEXES; ESCHERICHIA-COLI; ANTITUMOR-ACTIVITY; CIS; TRANS-DIAMMINEDICHLOROPLATINUM(II); COORDINATION; TRANS; TOXICITY; REPAIR; CIS-DICHLOROBIS(CYCLOALKYLAMINE)PLATINUM(II) AND TRANS-DICHLOROBIS(CYCLOALKYLAMINE)PLATINUM(II) COMPLEXES; ANTITUMOR ACTIVITY; MDA-MB-231 BREAST CANCER CELL LINE |
| Depositing User: | Dr. Gernot Deinzer |
| Last Modified: | 19 Oct 2022 08:42 |
| URI: | https://pred.uni-regensburg.de/id/eprint/53982 |
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