945893-19-6Relevant articles and documents
Tariquidar analogues: Synthesis by CuI-catalysed N/O-aryl coupling and inhibitory activity against the ABCB1 transporter
Egger, Michael,Li, Xuqin,Mueller, Christine,Bernhardt, Guenther,Buschauer, Armin,Koenig, Burkhard
, p. 2643 - 2649 (2007)
Less lipophilic and better water soluble tariquidar analogues were synthesised from one central anthranilic acid derived building block by Cu I-catalysed N/O-arylation reactions. The compounds were tested for their inhibitory activity against the ABCB1 transporter in a flow cytometric calcein-AM efflux assay. A correlation between their calculated log P values and their activities was observed, with the more lipophilic analogues being as potent as the reference substance tariquidar. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.