title: First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators.
abstract: A series of 3-benzyloxy-1-aza-9-oxafluorenes has been synthesized and biologically evaluated as novel MDR modulators. The concentration dependent inhibition of the efflux pump ABCB1 (P-glycoprotein) has been characterized and is discussed in relation to calculated lipophilicity data. Instead of the molecular lipophilicity the exact positioning of functional groups was found decisive for the biological activities.
authors.affiliation: Institute of Pharmacy, Martin-Luther University Halle-Wittenberg, Wolfgang-Langenbeck Str. 4, D-06120 Halle, Germany.
authors.forename: Martin
authors.initials: M
authors.lastname: Krug
authors.forename: Burkhardt
authors.initials: B
authors.lastname: Voigt
authors.forename: Christiane
authors.initials: C
authors.lastname: Baumert
authors.forename: Ralf
authors.initials: R
authors.lastname: Lüpken
authors.forename: Joséf
authors.initials: J
authors.lastname: Molnár
authors.forename: Andreas
authors.initials: A
authors.lastname: Hilgeroth
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000037:antagonists & inhibitors; D000818:Animals; D045744:Cell Line, Tumor; D055808:Drug Discovery; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D005449:Fluorenes / Q000737:chemistry* / Q000494:pharmacology*; D057927:Hydrophobic and Hydrophilic Interactions; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D005449:Fluorenes