Background: Natural occurring beta-Carbolines alkaloids are abundant in the plant kingdom or other organisms, and they were found to possess good antitumor activity through multiple mechanisms. Based on previous summarized SARs of beta-carboline derivatives, the modification on pyridine ring would have a great impact on their antitumor activities. Therefore, we plan to synthesized arylated beta -carboline-3-amides to find more valuable beta-Carbolines derivatives.Methods: A novel bimetallic Pd(OAc)(2)/AgOAc catalyst system was developed for the amidation of aryl iodides under acid condition. A series of N-arylated beta-carbolines derivatives were synthesized using this method. The structures of these compounds were confirmed by H-1 NMR, C-13 NMR and FIRMS, and their in vitro antiproliferative activity was investigated against HepG2 and Hela tumor cell lines by MTT assay.Results: Eleven N-arylated beta-carboline-3-amides were synthesized using this bimetallic catalyzed method in 58-98% yields. These synthesized N-arylated compounds showed no antiproliferative activity at 20 mu M.Conclusion: We have discovered an efficient and bimetallic catalytic system allowing the N-arylation of secondary acyclic amides. This is the first report that N-arylation of aliphatic secondary acyclic amides under acid condition.