Development of small-molecule P-gp inhibitors of the N-benzyl 1, 4-dihydropyridine type: novel aspects in SAR and bioanalytical evaluation of multidrug resistance ( …

…, S Krawczyk, M Hemmer, T Wersig, A Langner…

文献索引：Baumert, Christiane; Guenthel, Marianne; Krawczyk, Soeren; Hemmer, Marc; Wersig, Tom; Langner, Andreas; Molnar, Josef; Lage, Hermann; Hilgeroth, Andreas Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 1 p. 166 - 177

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被引用次数: 16

摘要

Novel series of N-benzyl 1, 4-dihydropyridines have been prepared by facile syntheses. All relevant substituents of the molecular scaffold have been varied. The resulting compounds were biologically evaluated as P-glycoprotein (P-gp) inhibitors. Substitutions of the N-benzyl residue favour biological activity beside respective 3-ester functions. Most active compounds were further evaluated as multidrug resistance (MDR) modulators to restore the cytotoxic ...