The synthesis, structural charaterization, antimicrobial activities and DNA interaction of bis-acridin ligands

The ways of fight against cancer have increased with emerging science and technology. One of these ways is to design a small molecule that can recognize, bind and cleave DNA in specific way. Recently, this way is become one of the most important and interesting subject in the field of bioorganic chemistry, biochemistry, biotechnology, and medicine. Cationic, flat and aromatic ethidium bromide and proflavine bind to DNA by inserting and intercalating between the base pairs of the double helix. However, bis-proflavine conjugated polyamide chain similar to N-methyl-pyrrole, N-methyl-imidazole and succinamide that bind to minor groove of DNA. Bis-intercalators incorporate two covalently attached intercalating ring systems to a polyamide chain of variable length. Therefore, bis-intercalating agents may offer several advantages according to mono-intercalating agents such as, higher binding affinity, much more biological activity and more selectivity, we became interested to synthesise the bis-intercalating agents. With this aim, two bis-intercalation molecules of different chain lengths (41 and 52) have been synthesized and characterized. The DNA cleavage activities were determined by Agarose Jel Electrophoresis in the absence and presence of Cupper(II). It was observed that DNA strand scission was increased with the increased concentration of ligands. By comparision the antimicrobial activity of ligands with standart antibiotics, the ligands showed moderate inhibition against tested microorganisms.