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Benzanilide – Biphenyl Replacement: A Bioisosteric Approach to Quinoline Carboxamide-type ABCG2 Modulators

Ochoa-Puentes, Cristian ; Bauer, Stefanie ; Kühnle, Matthias ; Bernhardt, Günther ; Buschauer, Armin ; König, Burkhard


Recently reported compounds such as UR-COP78 (6) are among the most potent and selective ABCG2 modulators known so far, but prone to rapid enzymatic cleavage at the central benzanilide moiety. In search for more stable analogs, according to a bioisosteric approach, a series of N-(biphenyl-3-yl)quinoline carboxamides was prepared by solid phase and solution phase synthesis. The biphenyl moiety was ...


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