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Published on: June 23, 2019
Synthesis and biological activities of topopyrones
Paul A Zaleski1, Rumit Maini, Simon J Leiris
1Center for BioEnergetics, Biodesign Institute, Arizona State University, Tempe, Arizona 85287-6301, USA.
Abstract:
Structure-activity studies were employed to investigate the stabilization of DNA-topoisomerases I and II covalent binary complexes by topopyrone analogues. The synthesis of five new topopyrone derivatives and study of their ability to stabilize DNA-topoisomerase I and DNA-topoisomerase II covalent binary complexes are described. The biochemical assays suggest that the orientation of the fused 1,4-pyrone ring and halogen substituents contribute importantly to the overall potency of the topopyrones as topoisomerase poisons.
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