Discovery of 9,10-dihydroacridines as novel class of ABCB1 inhibitors

Andreas Hilgeroth, Marc Hemmer, Sebastian Neuber, Josef Molnár, Hermann Lage

Research output: Contribution to journalArticle

Abstract

Nonplanar 9,10-dihydroacridines were synthesized as promising C2 symmetric molecular scaffolds as inhibitors of the transmembrane efflux pump ABCB1. Within the series structure-activity relationships are discussed revealing the importance of hydrogen bond acceptor functions. A selectivity of ABCB1 inhibition is demonstrated for selected candidates and a bioanalytical study proved nontoxicity as well as missing ABCB1 substrate properties. The results encourage to further develop the promising class of ABCB1 inhibitors.

Original languageEnglish
Pages (from-to)329-335
Number of pages7
JournalMedicinal Chemistry
Volume11
Issue number4
DOIs
Publication statusPublished - Jan 1 2015

Keywords

  • ABCB1 inhibitor
  • ABCB1 substrate properties
  • Structure-activity relationships

ASJC Scopus subject areas

  • Drug Discovery

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