Synthesis and biological activity of N-aroyl-tetrahydro-γ-carbolines

Research on dual inhibitors of both 5-LOX and COXs gained interest due to the overexpressions of these enzymes during the malignant state of the evolution of prostate cancer. In order to take part in this research, new N-aroyl-tetrahydro-γ-carbolines issued from the modification of Indomethacin have been synthesised. As for the NSAIDs, the compounds have been tested for their activity against COX1, COX2 plus against 5-LOX and against the proliferation of malignant prostate cancer. Interesting cytotoxic activities and selectivities of some tetrahydro-γ-carboline derivatives have been obtained.

Tetrahydro-γ-carboline derivatives exhibited potent inhibitory activity with IC50 values in the range of 3.0–6.0 μM.Figure optionsDownload as PowerPoint slide