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Synthesis and biological activities of topopyrones. | LitMetric

Synthesis and biological activities of topopyrones.

J Nat Prod

Center for BioEnergetics, Biodesign Institute, Arizona State University, Tempe, Arizona 85287-6301, USA.

Published: April 2012

AI Article Synopsis

Article 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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http://dx.doi.org/10.1021/np200777zDOI Listing

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