5-Methyl-Benzofuro[3,2-<i>b</i>]quinoline Derivatives as DNA Binders

Abstract

Several derivatives of 5-methyl-benzofuro [3,2-quinoline (O-isostere of cryptolepine) were synthesized. Spectrometric experiments and molecular modeling indicated that these derivatives interacted with duplex DNA by intercalation binding mode. The derivatives with aniline substituent exhibited superior DNA binding affinity to that of lead compound 5-methyl-benzofuro [3,2-quinoline.