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

Bioorg Med Chem. 2013 Jan 1;21(1):166-77. doi: 10.1016/j.bmc.2012.10.041.

Christiane Baumert ¹, Marianne Günthel, Sören Krawczyk, Marc Hemmer, Tom Wersig, Andreas Langner, Joséf Molnár, Hermann Lage, Andreas Hilgeroth

Affiliations

Affiliation

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

PMID: 23199479 DOI: 10.1016/j.bmc.2012.10.041

Abstract

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.

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