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Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar

Kühnle, Matthias ; Egger, Michael ; Müller, Christine ; Mahringer, Anne ; Bernhardt, Günther ; Fricker, Gert ; König, Burkhard ; Buschauer, Armin



Abstract

The efflux pumps ABCB1 (p-gp, MDR1) and ABCG2 (BCRP) are expressed to a high extent by endothelial cells at the blood-brain barrier (BBB) and other barrier tissues, and are involved in drug resistance of tumor (stem) cells. Whereas numerous ABCB1 inhibitors are known, only a few ABCG2 modulators with submicromolar activity have been published. Starting from tariquidar (4) analogs as ABCB1 ...

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