Z1-6735 — Annual report 2015
1.
Ruthenium complexes as inhibitors of 15-lipoxygenase-1

The paper presents the synthesis and thorough characterization of three new and two previously published ruthenium complexes. These compounds as well as the ruthenium precursors and the respective ligands (11 compounds in total) were tested as inhibitors of 15-lipoxygenase-1, an enzyme that catalyses the stereospecific insertion of oxygen into polyunsaturated fatty acids and represents a therapeutic target for inflammatory diseases. A complex bearing a pyridine-N-oxide ligand was found to be a potent inhibitor with IC50 vales in the near-nanomolar range.

COBISS.SI-ID: 1536536259
2.
Structure-related mode-of-action differences of anticancer organoruthenium complexes with ß-diketonates

The paper presents the study on the mode-of-action differences of two series of anticancer ruthenium complexes bearing diketone ligands. One series, bearing labile chlorido ligands was found to be highly toxic while the series bearing substitutionally inert phosphine pta was found to be strongly cytostatic as evidenced by cell cycle analysis and ruthenium cellular accumulation.

COBISS.SI-ID: 1536265667
3.
Ruthenium complexes as inhibitions of the aldo-keto reductases AKR1C1-1C3

A series of nitrogen chelating agents and their ruthenium complexes were tested as inhibitors of AKR1C1-3 enzymes. The complex bearing a benzothiazole ligand was found to be a potent irreversible inhibitor with IC50 values in the low micromolar range.

COBISS.SI-ID: 31698649