Discovery of pyridine-2-ones as novel class of multidrug resistance (MDR) modulators: First structure-activity relationships

Sören Krawczyk, Monika Otto, Alexander Otto, Claudius Coburger, Martin Krug, Marianne Seifert, Volkmar Tell, Joséf Molnár, Andreas Higeroth

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

A novel facile synthesis led to pyridine-2-one target structures of which first series with varying substituents have been yielded and biologically characterized as novel multidrug resistance (MDR) modulators inhibiting P-glycoprotein (P-gp). Structure-activity relationships prove a dependency of the MDR-modulating properties from the kind and positioning of hydrogen bond acceptor functions within the molecular skeleton. Cyano functions turned out as biologically effective substituents for a potential hydrogen bonding to the protein target structure.

Original languageEnglish
Pages (from-to)6309-6315
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number21
DOIs
Publication statusPublished - Nov 1 2011

Keywords

  • Efflux pump inhibition
  • Lead structure
  • Multidrug resistance (MDR)
  • P-glycoprotein (P-gp)
  • Structure-activity relationships (SAR)

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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