Title:Discovery of 9,10-Dihydroacridines as Novel Class of ABCB1 Inhibitors
Volume: 11
Issue: 4
Author(s): Andreas Hilgeroth, Marc Hemmer, Sebastian Neuber, Josef Molnar and Hermann Lage
Affiliation:
Keywords:
ABCB1 inhibitor, ABCB1 substrate properties, structure-activity relationships.
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.