Synthese und Untersuchung lipophiler Platinverbindungen [article]

Christian Paetz, Martin-Luther Universität, Universitäts- Und Landesbibliothek Sachsen-Anhalt
The present work deals with the subject of synthesis and cytostatic testing of lipophilic Cisplatin and Carboplatin derivatives. Starting from halogene alcohols with varying chainlengths, multistep sytheses afforded the preparation of diamine structures with the terminal substituents cholic acid, the THP protection group or the free hydroxy function. All diamin chelators were subjected to react with the platinum moiety in the last step of the synthesis. The examination of the cytotoxicity was
more » ... cytotoxicity was accomplished by using the sulforhodamine-B (SRB) assay against a human squamous carcinoma cell line (UM-SCC- 22B). The examinations revealed that cholic acid platinum compounds show a strong cytotoxic effect in suspension, but not at all in saturated concentrations. On the other hand the symmetric and asymmetric propandiamine compounds were more soluble and were proved to have a strong cytotoxicity in solution. The analogous ethylene diamine structures as well as the compounds with a free terminal hydroxyl group had no effect on the examinated cell line.
doi:10.25673/3463 fatcat:pbirtockvfeqdogaupqme6z6em