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Updated: Apr 21, 2026

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Discovery of 9,10-Dihydroacridines as Novel Class of ABCB1 Inhibitors
Andreas Hilgeroth, Marc Hemmer, Sebastian Neuber
1Institute of Pharmacy, Martin- Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany. andreas.hilgeroth@pharmazie.uni-halle.de.
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.
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