Abstract

Three groups of distamycin analogues containing benzene units, potential minor groove binders, each containing six compounds, have been synthesized using Syncore Reactor. Ethidium bromide assay was used to show that these compounds bind to plasmid pBR322. The most active in fluorescence reduction appeared to be compounds with configuration meta-meta of benzene rings, formed library D.

Keywords: Combinatorial chemistry, Distamycin analogues, DNA binding, Parallel synthesis, Solid phase synthesis, meta-meta, benzene rings, DNA, helical curve, B-DNA, distamycin, Streptomyces distallicus, nitroamines, solid-phase syntheses, Ethidium bromide displacement assay