Myxochelin-Inspired 5-Lipoxygenase Inhibitors: Synthesis and Biological Evaluation.
Sebastian SchieferdeckerStefanie KönigSimona PaceOliver WerzMarkus NettPublished in: ChemMedChem (2016)
A total of 48 analogues of the natural product myxochelin A were prepared and evaluated for their inhibitory effects on human 5-lipoxygenase in both cell-free and cell-based assays. Structure-activity relationship analysis revealed that the secondary alcohol function and only chiral center of myxochelin A is not required for biological activity. By expanding the diaminoalkane linker of the two aromatic residues it was possible to generate a myxochelin derivative with superior activity against 5-lipoxygenase in intact cells.
Keyphrases
- structure activity relationship
- cell free
- single cell
- induced apoptosis
- endothelial cells
- cell cycle arrest
- high throughput
- cell therapy
- induced pluripotent stem cells
- molecular docking
- endoplasmic reticulum stress
- stem cells
- pluripotent stem cells
- oxidative stress
- ionic liquid
- alcohol consumption
- capillary electrophoresis
- data analysis