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Discovery of 9,10-Dihydroacridines as Novel Class of ABCB1 Inhibitors

[ Vol. 11 , Issue. 4 ]

Author(s):

Andreas Hilgeroth, Marc Hemmer, Sebastian Neuber, Josef Molnar and Hermann Lage   Pages 329 - 335 ( 7 )

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.

Keywords:

ABCB1 inhibitor, ABCB1 substrate properties, structure-activity relationships.

Affiliation:

Institute of Pharmacy, Martin- Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.

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