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


CONCLUSIONS
Eudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain.
Department of Medicinal Chemistry, College of Pharmacy, Fudan University, Shanghai 200032, China.
Xiao-chun
XC
Dong
Ren
R
Wen
Jian-bin
JB
Zheng
D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D007211:Indoles; D007941:Leukemia P388 / Q000473:pathology; D051379:Mice; D015394:Molecular Structure; D014363:Tryptamines
D000470:Alkaloids; D000970:Antineoplastic Agents; D002243:Carbolines; D007211:Indoles; D014363:Tryptamines; C088110:eudistomin U; C030820:tryptamine; C012381:indole-3-carbaldehyde