Abstract
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, ...
Abstract
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. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007).
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