Ellipticine analogues and related compounds as inhibitors of reverse transcriptase and as inhibitors of the efflux pump

Derek Sharples, György Hajós, Zsuzsanna Riedl, Dorottya Csnyi, József Molnr, Diana Szabó

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

Ten polycyclic derivatives related to ellipticine have been synthesised and tested for their intercalating, reverse transcriptase (RT) inhibitory and multidrug resistance efflux pump inhibitory properties. The intercalating activity and the RT inhibitory activity of the derivatives suggest that ellipticine analogues bind at an allosteric binding site on RT or that this inhibition could be controlled at the DNA level. The MDR efflux pump inhibitory activities of these derivatives, however, appears to be unrelated to the DNA binding ability.

Original languageEnglish
Pages (from-to)269-274
Number of pages6
JournalArchiv der Pharmazie
Volume334
Issue number8-9
DOIs
Publication statusPublished - Jan 1 2001

Keywords

  • Efflux pump
  • Ellipticine
  • Heterocycles
  • Intercalation
  • Multidrug resistance

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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