title: Novel structurally varied N-alkyl 1,4-dihydropyridines as ABCB1 inhibitors: structure-activity relationships, biological activity and first bioanalytical evaluation.
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.
authors.affiliation: Institute of Pharmacy, Martin- Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany. andreas.hilgeroth@pharmazie.uni-halle.de
authors.forename: Andreas
authors.initials: A
authors.lastname: Hilgeroth
authors.forename: Christiane
authors.initials: C
authors.lastname: Baumert
authors.forename: Claudius
authors.initials: C
authors.lastname: Coburger
authors.forename: Marianne
authors.initials: M
authors.lastname: Seifert
authors.forename: Sören
authors.initials: S
authors.lastname: Krawczyk
authors.forename: Cornelius
authors.initials: C
authors.lastname: Hempel
authors.forename: Felix
authors.initials: F
authors.lastname: Neubauer
authors.forename: Martin
authors.initials: M
authors.lastname: Krug
authors.forename: Josef
authors.initials: J
authors.lastname: Molnár
authors.forename: Hermann
authors.initials: H
authors.lastname: Lage
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D004095:Dihydropyridines / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004095:Dihydropyridines; D011804:Quinolines