Synthesis and biological activities of topopyrones

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

Research output: Contribution to journalArticle

13 Citations (Scopus)

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

Fingerprint

Type II DNA Topoisomerase
Type I DNA Topoisomerase
Bioactivity
Pyrones
Halogens
Poisons
Assays
Stabilization
Derivatives

ASJC Scopus subject areas

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

Cite this

Zaleski, P. A., Maini, R., Leiris, S. J., Elban, M. A., & Hecht, S. (2012). Synthesis and biological activities of topopyrones. Journal of Natural Products, 75(4), 577-585. https://doi.org/10.1021/np200777z

Synthesis and biological activities of topopyrones. / Zaleski, Paul A.; Maini, Rumit; Leiris, Simon J.; Elban, Mark A.; Hecht, Sidney.

In: Journal of Natural Products, Vol. 75, No. 4, 27.04.2012, p. 577-585.

Research output: Contribution to journalArticle

Zaleski, PA, Maini, R, Leiris, SJ, Elban, MA & Hecht, S 2012, 'Synthesis and biological activities of topopyrones', Journal of Natural Products, vol. 75, no. 4, pp. 577-585. https://doi.org/10.1021/np200777z
Zaleski, Paul A. ; Maini, Rumit ; Leiris, Simon J. ; Elban, Mark A. ; Hecht, Sidney. / Synthesis and biological activities of topopyrones. In: Journal of Natural Products. 2012 ; Vol. 75, No. 4. pp. 577-585.
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