Original cytotoxic bisindole alkaloids with a 1,2,3,4-tetrahydroquinoline b
ridge were synthesized by reductive amination with various anilines. The mo
st cytotoxic compounds display a high and dose-dependent cell cycle effect
with accumulation in the G1 phase. Influence of substitution of the startin
g aniline on the reaction and on cytotoxicity of produced dimers was pointe
d out. (C) 2000 Elsevier Science Ltd. All rights reserved.