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Solid phase synthesis of tariquidar-related modulators of ABC transporters preferring breast cancer resistance protein (ABCG2)

Ochoa Puentes, Cristian ; Höcherl, Peter ; Kühnle, Matthias ; Bauer, Stefanie ; Kürger, Kira ; Bernhardt, Günther ; Buschauer, Armin ; König, Burkhard



Abstract

Aiming at structural optimization of potent and selective ABCG2 inhibitors, such as UR-ME22-1, from our laboratory, an efficient solid phase synthesis was developed to get convenient access to this class of compounds. 7-Carboxyisatoic anhydride was attached to Wang resin to give resin bound 2-aminoterephthalic acid. Acylation with quinoline-2- or -6-carbonyl chlorides, coupling with ...

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