First biological evaluation of developed 3-benzyloxyfluorenes as novel class of MDR modulators

被引：8

作者：

Krug, Martin ^{[1
]}

Voigt, Burkhardt ^{[1
]}

Baumert, Christiane ^{[1
]}

Luepken, Ralf ^{[1
]}

Molnar, Josef ^{[2
]}

Hilgeroth, Andreas ^{[1
]}

机构：

[1] Univ Halle Wittenberg, Inst Pharm, D-06120 Halle, Germany

[2] Univ Szeged, Dept Med Microbiol, H-6720 Szeged, Hungary

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 06期

关键词：

ABCB1; inhibitor; Efflux pump; MDR modulator; Binding site; Lipophilicity calculation; MULTIDRUG-RESISTANCE; TRANSPORTERS;

D O I：

10.1016/j.ejmech.2010.02.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：2683 / 2688

页数：6

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