Synthesis and COX Inhibitory Activities of Rutaecarpine Derivatives

A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity (IC 5 0 = 0.27, 0.35 μM, respectively) with selectivity.