Investigation of effects of ellipticine derivatives on human DNA topoisomerases enzymes

DNA topoisomerases are among the most important group of enzymes having vital cellular roles in replication, transcription and recombination. These enzymes change the three dimensional structure of DNA without affecting chemical structure through transient breaks. Topoisomerases, which are classified as type I and type II according to whether they produce single or double strand breaks in their reaction mechanisms are qualified as popular targets for anticancer drugs. In particular, topoisomerase II enzyme that belongs to type II class comprises preferential targets in chemotherapy due to their roles in cellular proliferation. In this study, newly synthesized ellipticine derivatives were investigated to assess their effects on topoisomerases. Their effects on main reactions of topoisomerases, relaxation and decatenation, have been examined with the experiments to reveal whether they affect the rate of DNA cleavage by topoisomerases. Our study was detailed by investigating their intercalative properties.