First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators.
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.
Krug
Martin
M
Institute of Pharmacy, Martin-Luther University Halle-Wittenberg, Wolfgang-Langenbeck Str. 4, D-06120 Halle, Germany.
Voigt
Burkhardt
B
Baumert
Christiane
C
Lüpken
Ralf
R
Molnár
Joséf
J
Hilgeroth
Andreas
A
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
D018435:ATP Binding Cassette Transporter, Subfamily B; D005449:Fluorenes