Novel insight in structure-activity relationship and bioanalysis of p-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes

被引：24

作者：

Coburger, Claudius ^{[1
]}

Wollmann, Joerg ^{[1
]}

Baumert, Christiane ^{[1
]}

Krug, Martin ^{[1
]}

Molnar, Josef ^{[2
]}

Lage, Hermann ^{[3
]}

Hilgeroth, Andreas ^{[1
]}

机构：

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

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

[3] Univ Hosp Charite, Inst Pathol, D-10117 Berlin, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 18期

关键词：

D O I：

10.1021/jm800480y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 3,9-diazatetraasteranes have been synthesized with varied aromatic substitution patterns and evaluated as P-glycoprotein (P-gp) inhibitors. Structure-activity relationships (SAR) are discussed in relation to determined physicochemical properties. The potential to induce P-gp expression has been evaluated in cancer cell lines. The bioanalytical results indicate favorable noninducing properties compared to P-gp inducing drug standard.

引用

页码：5871 / 5874

页数：4

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