Novel Structurally Varied N-Alkyl 1,4-Dihydropyridines as ABCB1 Inhibitors: Structure-Activity Relationships, Biological Activity and First Bioanalytical Evaluation

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.

Cite this article as:

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