[Synthesis of 1-indole substituted beta-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities].

AIM

To synthesize eudistomin U and its 6-OCH3/Br derivatives and 5'-Br derivatives as antitumor agents.

METHODS

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.

RESULTS

The structures of the compounds were determined by 1HNMR, MS and HRMS. Antitumor activity in vitro was tested.

CONCLUSION

Eudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain.