Synthesis of 1-indole substituted beta-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities / 药学学报

ABSTRACT

<p><b>AIM</b>To synthesize eudistomin U and its 6-OCH3/Br derivatives and 5'-Br derivatives as antitumor agents.</p><p><b>METHODS</b>Using tryptamine and indole-3-aldehyde as starting materials, through condensation, Pictet-Spengler cyclization and dehydrogenation three steps, the alkaloids and its derivatives were prepared.</p><p><b>RESULTS</b>The structures of the compounds were determined by 1HNMR, MS and HRMS. Antitumor activity in vitro was tested.</p><p><b>CONCLUSION</b>Eudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain.</p>