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  • Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.

Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.

Bioorganic & medicinal chemistry (2010-05-11)
Alexandre Bridoux, Régis Millet, Jean Pommery, Nicole Pommery, Jean-Pierre Henichart
ABSTRACT

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-gamma-carbolines issued from the modification of Indomethacin have been synthesised. As for the NSAIDs, the compounds have been tested for their activity against COX(1), COX(2) plus against 5-LOX and against the proliferation of malignant prostate cancer. Interesting cytotoxic activities and selectivities of some tetrahydro-gamma-carboline derivatives have been obtained.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Indomethacin, 98.0-102.0%, meets EP testing specifications
Sigma-Aldrich
Indomethacin, meets USP testing specifications