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

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.

Cite this article as:

Hilgeroth Andreas, Hemmer Marc, Neuber Sebastian, Molnar Josef and Lage Hermann, Discovery of 9,10-Dihydroacridines as Novel Class of ABCB1 Inhibitors, Medicinal Chemistry 2015; 11 (4) . https://dx.doi.org/10.2174/1573406410666141111100720