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

Author(s): Andreas Hilgeroth, Christiane Baumert, Claudius Coburger, Marianne Seifert, Soren Krawczyk, Cornelius Hempel, Felix Neubauer, Martin Krug, Josef Molnar, Hermann Lage.

Journal Name: Medicinal Chemistry

Volume 9 , Issue 4 , 2013

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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

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Article Details

VOLUME: 9
ISSUE: 4
Year: 2013
Page: [487 - 493]
Pages: 7
DOI: 10.2174/1573406411309040002
Price: $58

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