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 (MDR) reversal properties.

Christiane Baumert, Marianne Günthel, Sören Krawczyk, Marc Hemmer, Tom Wersig, Andreas Langner, Joséf Molnár, Hermann Lage, Andreas Hilgeroth

Institute of Pharmacy, Martin Luther University, 06120 Halle, Germany.

Bioorganic & medicinal chemistry 2013 Jan 1

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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 properties of varying daunorubicin applications. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Christiane Baumert, Marianne Günthel, Sören Krawczyk, Marc Hemmer, Tom Wersig, Andreas Langner, Joséf Molnár, Hermann Lage, Andreas Hilgeroth. 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 (MDR) reversal properties. Bioorganic & medicinal chemistry. 2013 Jan 1;21(1):166-77