Synthesis and biological activity of N-aroyl-tetrahydro-gamma-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-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.
Bridoux
Alexandre
A
Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université Lille-Nord de France, 59006 Lille, France. abridoux@wanadoo.fr
Millet
Régis
R
Pommery
Jean
J
Pommery
Nicole
N
Henichart
Jean-Pierre
JP
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007213:Indomethacin; D016859:Lipoxygenase Inhibitors; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002243:Carbolines; D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors; C055572:gamma-carboline; D007213:Indomethacin