Synthesis and Biological Evaluation of Novel β-Carbolines as Potent Cytotoxic and DNA Intercalating Agents

Abstract

A series of novel water-soluble β-carbolines bearing a flexible amino side chain was designed, synthesized and evaluated as potent cytotoxic and DNA intercatalating agents. The N⁹-arylated alkyl substituted β-carbolines represented the most interesting cytotoxic activities. The results suggested that (1) the N⁹-arylated alkyl substituents of β-carboline nucleus played a very important role in the modulation of the cytotoxic potencies; (2) the length of the alkylamino side chain significantly affected their cytotoxic potency, and N,N-dimethylaminopropylamino substituent were more favorable. In addition, these compounds were found to exhibit significant DNA intercalating potencies.