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 |
| |
| Authors: | Christiane Baumert Marianne Günthel Sören Krawczyk Marc Hemmer Tom Wersig Andreas Langner Joséf Molnár Hermann Lage Andreas Hilgeroth |
| |
| Affiliation: | 1. Institute of Pharmacy, Martin Luther University, 06120 Halle, Germany;2. Department of Medical Microbiology, University of Szeged, 6720 Szeged, Hungary;3. Institute of Pathology, University Hospital Charité, 10117 Berlin, Germany |
| |
| 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. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
