Synthesis of novel β-carbolines with efficient DNA-binding capacity and potent cytotoxicity

Abstract

A series of water-soluble β-carbolines, bearing a flexible amino side chain, was prepared and evaluated in vitro against a panel of human tumor cell lines. The N 9-arylated alkyl substituted β-carbolines represented the most interesting cytotoxic activities, and compound 7b was found to be the most potent antitumor agent with IC 50 values lower than 10 μM against eight human tumor cell lines. The results confirmed that the N 9-arylated alkyl substituents of β-carboline nucleus played an important role in the modulation of the cytotoxic potencies. In addition, these compounds were found to exhibit significant DNA-binding affinity.