Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4-
dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed.
Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has
been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of
ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.
Keywords: ABCB1 inhibitor, structure-activity relationships, ABCB1 substrate properties
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