Synthesis and biological activities of topopyrones

Paul A. Zaleski, Rumit Maini, Simon J. Leiris, Mark A. Elban, Sidney Hecht

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)577-585
Number of pages9
JournalJournal of Natural Products
Volume75
Issue number4
DOIs
StatePublished - Apr 27 2012

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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