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

[ Vol. 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   Pages 487 - 493 ( 7 )

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

Affiliation:

Institute of Pharmacy, Martin- Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.



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