Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties

被引：26

作者：

Brachwitz, K ^{[1
]}

Voigt, B ^{[1
]}

Meijer, L ^{[1
]}

Lozach, P ^{[1
]}

Schächtele, C ^{[1
]}

Molnár, J ^{[1
]}

Hilgeroth, A ^{[1
]}

机构：

[1] Univ Halle Wittenberg, Inst Pharmaceut Chem, D-06120 Halle Saale, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 05期

关键词：

D O I：

10.1021/jm021090g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The first series of synthetic 1-aza-9-oxafluorenes with cytostatic activities in the micromolar range was evaluated as cyclin-dependent kinase (CDK1) inhibitors. Activity was found to be selective in comparison to the inhibition of other kinases within the CDK family. Compounds were shown to inhibit the membrane-efflux pump P-glycoprotein responsible for multidrug resistance in cancer cells. First structure-activity relationships are discussed.

引用

页码：876 / 879

页数：4

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