Abstract
Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.
Keywords: ABCB1 inhibitor, structure-activity relationships, ABCB1 substrate properties
Medicinal Chemistry
Title:Novel Structurally Varied N-Alkyl 1,4-Dihydropyridines as ABCB1 Inhibitors: Structure-Activity Relationships, Biological Activity and First Bioanalytical Evaluation
Volume: 9 Issue: 4
Author(s): Andreas Hilgeroth, Christiane Baumert, Claudius Coburger, Marianne Seifert, Soren Krawczyk, Cornelius Hempel, Felix Neubauer, Martin Krug, Josef Molnar and Hermann Lage
Affiliation:
Keywords: ABCB1 inhibitor, structure-activity relationships, ABCB1 substrate properties
Abstract: Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.
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Hilgeroth Andreas, Baumert Christiane, Coburger Claudius, Seifert Marianne, Krawczyk Soren, Hempel Cornelius, Neubauer Felix, Krug Martin, Molnar Josef and Lage Hermann, Novel Structurally Varied N-Alkyl 1,4-Dihydropyridines as ABCB1 Inhibitors: Structure-Activity Relationships, Biological Activity and First Bioanalytical Evaluation, Medicinal Chemistry 2013; 9 (4) . https://dx.doi.org/10.2174/1573406411309040002
DOI https://dx.doi.org/10.2174/1573406411309040002 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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