Egger, Michael, Li, Xuqin, Müller, Christine, Bernhardt, Günther, 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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Other URL: http://www3.interscience.wiley.com/cgi-bin/abstract/114215593/ABSTRACT
Abstract
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.
Export bibliographical data
| Item type: | Article | ||||
|---|---|---|---|---|---|
| Date: | 2007 | ||||
| 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 | ||||
| Identification Number: |
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| Keywords: | Cross-coupling; Medicinal chemistry; Lipophilicity | ||||
| Dewey Decimal Classification: | 500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 3379 |
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