Egger, Michael and Li, Xuqin and Mueller, Christine and Bernhardt, Guenther and Buschauer, Armin and Koenig, Burkhard (2007) Tariquidar analogues: Synthesis by Cu-I-catlyzed N/O-aryl coupling and inhibitory activity against the ABCB1 transporter. EUROPEAN JOURNAL OF ORGANIC CHEMISTRY (16). pp. 2643-2649. ISSN 1434-193X, 1099-0690
Full text not available from this repository. (Request a copy)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).
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | PALLADIUM-CATALYZED AMINATION; N BOND FORMATION; MULTIDRUG-RESISTANCE; P-GLYCOPROTEIN; BRAIN; BROMIDES; CHLORIDES; REVERSAL; HALIDES; EFFLUX; cross-coupling; medicinal chemistry; lipophilicity |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 07 Dec 2020 14:44 |
| Last Modified: | 08 Dec 2020 15:38 |
| URI: | https://pred.uni-regensburg.de/id/eprint/32649 |
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