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

作者：Hilgeroth Andreas^*; Baumert Christiane; Coburger Claudius; Seifert Marianne; Krawczyk Soeren; Hempel Cornelius; Neubauer Felix; Krug Martin; Molnar Josef; Lage Hermann

来源：Medicinal Chemistry, 2013, 9(4): 487-493.

DOI：10.2174/1573406411309040002

• ABCB1 inhibitor
• structure-activity relationships
• ABCB1 substrate properties

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.

• 出版日期2013-6