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Abstract
The development of novel biologically active organometallic compounds bearing an acetylsalicylic acid (ASA) substructure led to the synthesis of analogical Zeise-type salts that accordingly inhibit cyclooxygenase (COX) enzymes. In order to determine the influence of the length of the alkyl chain between the platinum(II) center and the ASA moiety, compounds with varying methylene groups (n = 1–4) were synthesized and characterized. For the propene derivative structural elucidation by X-ray crystallography was possible. Prior to evaluation of biological activity, the complexes were investigated regarding their stability in different media, such as water, physiological sodium chloride, and phosphate buffered saline. Therefore, an analytical method based on capillary electrophoresis was established. All of the compounds were tested for their COX inhibitory potential. In general, complexes with longer alkyl chains caused higher inhibition of COX enzymes and the inhibitory potential towards COX enzymes was enhanced when compared to Zeise’s salt. The growth inhibitory effects of the synthesized substances were investigated in vitro against colon carcinoma (HT-29) and breast cancer (MCF-7) cells. The IC50 values of the new derivatives ranged from 30 to 50 µM, whereas neither Zeise’s salt itself nor ASA showed any antiproliferative activity at the used concentrations.
Highlights
The most famous platinum complex in anticancer therapy by far is Cisplatin, which was first synthesized by M
The IC50 values of the new derivatives ranged from 30 to 50 μM, whereas neither Zeise’s salt itself nor acetylsalicylic acid (ASA) showed any antiproliferative activity at the used concentrations
Carboplatin, and Oxaliplatin (Figure 1) have in common that they are restricted by dose limiting side effects as well as frequent development of resistance
Summary
The most famous platinum complex in anticancer therapy by far is Cisplatin, which was first synthesized by M. Peyrone in 1844 [1] It took more than 120 years until its antitumor effect was discovered by B. Various derivatives of Cisplatin were synthesized that differ in the leaving groups and/or in the carrier ligands to improve its pharmacological profile. Only a few derivatives, such as Carboplatin and Oxaliplatin, are approved for tumor therapy [3,4,5]. Carboplatin, and Oxaliplatin (Figure 1) have in common that they are restricted by dose limiting side effects as well as frequent development of resistance
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