Andreas Hilgeroth, Marc Hemmer, Sebastian Neuber, Josef Molnar and Hermann Lage Pages 329 - 335 ( 7 )
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.
ABCB1 inhibitor, ABCB1 substrate properties, structure-activity relationships.
Institute of Pharmacy, Martin- Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.