Synthesis of 1-indole substituted β-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities

AimTo synthesize eudistomin U and its 6-OCH₃/Br derivatives and 5′-Br derivatives as antitumor agents. MethodsUsing tryptamine and indole-3-aldehyde as starting materials, through condensation, Pictet-Spengler cyclization and dehydrogenation three steps, the alkaloids and its derivatives were prepared. ResultsThe structures of the compounds were determined by ₁HNMR, MS and HRMS. Antitumor activity in vitro was tested. ConclusionEudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain.