Egger, Michael and Li, Xuqin and Müller, Christine and Bernhardt, Günther and Buschauer, Armin and König, Burkhard (2007) Tariquidar analogues: synthesis by Cu(I)-catalysed N/O–aryl coupling and inhibitory activity against the ABCB1 transporter. European Journal of Organic Chemistry 2007 (16), pp. 2643-2649.
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Less lipophilic and better water soluble tariquidar analogues were synthesised from one central anthranilic acid derived building block by CuI-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.
|Institutions:|| Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König|
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
|Projects:||GRK 760, Graduiertenkolleg Medizinische Chemie|
|Keywords:||Cross-coupling; Medicinal chemistry; Lipophilicity|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||21 Feb 2008 08:09|
|Last Modified:||08 Nov 2010 15:12|