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Inhibition of ABC transporters associated with multidrug resistance

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Egger, Michael
Date of publication of this fulltext: 10 May 2010 08:52

Abstract (English)

The first part of this dissertation (chapters 1 and 2) deals with the inhibition of the ABC transporters ABCB1 (p-glycoprotein) and ABCG2 (breast cancer resistance protein). Less lipophilic and better water soluble analogues of the known ABCB1 inhibitor tariquidar were synthesized from one central building block via Cu(I)-catalyzed N/O-arylation reactions. These compounds were tested for their ...


Translation of the abstract (German)

Im ersten Teil dieser Arbeit (Kapitel 1 und 2) wird die Hemmung der ABC-Transporter ABCB1 (p-Glycoprotein) und ABCG2 (breast cancer resistance protein) beschrieben. Ausgehend von einer zentralen Vorstufe wurden durch Cu(I)-katalysierte N- und O-Arylierungen weniger lipophile und besser wasserlösliche Analoga des ABCB1-Inhibitors Tariquidar synthetisiert. Die inhibitorische Aktivität dieser neuen ...


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