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Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP)

Antoni, Frauke ; Bause, Manuel ; Scholler, Matthias ; Bauer, Stefanie ; Stark, Simone Alexandra ; Jackson, Scott M. ; Manolaridis, Ioannis ; Locher, Kaspar P. ; König, Burkhard ; Buschauer, Armin ; Bernhardt, Günther


Tariquidar derivatives have been described as potent and selective ABCG2 inhibitors. However, their susceptibility to hydrolysis limits their applicability. The current study comprises the synthesis and characterization of novel tariquidar-related inhibitors, obtained by bioisosteric replacement of the labile moieties in our previous tariquidar analog UR-ME22-1 (9). CuAAC ("click" reaction) gave ...


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