Small-Molecule Inhibitors of NADPH Oxidase 4

被引：47

作者：

Borbely, Gabor ^{[1
,2
]}

Szabadkai, Istvan ^{[1
]}

Horvath, Zoltan ^{[1
]}

Marko, Peter ^{[1
]}

Varga, Zoltan ^{[1
]}

Breza, Nora ^{[1
]}

Baska, Ferenc ^{[1
,2
]}

Vantus, Tibor ^{[4
]}

Huszar, Monika ^{[4
]}

Geiszt, Miklos ^{[5
]}

Hunyady, Laszlo ^{[5
]}

Buday, Laszlo ^{[6
]}

Orfi, Laszlo ^{[1
,2
,3
]}

Keri, Gyoergy ^{[1
,2
,4
]}

机构：

[1] Vichem Chem Res Ltd, Budapest, Hungary

[2] Semmelweis Univ, Rat Drug Design Lab CRC, H-1085 Budapest, Hungary

[3] Semmelweis Univ, Dept Pharmaceut Chem, H-1085 Budapest, Hungary

[4] Semmelweis Univ, Dept Med Chem, Hungarian Acad Sci, Pathobiochem Res Grp, H-1085 Budapest, Hungary

[5] Semmelweis Univ, Fac Med, Dept Physiol, H-1085 Budapest, Hungary

[6] Hungarian Acad Sci, Biol Res Ctr, Inst Enzymol, Budapest, Hungary

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 18期

关键词：

TYROSINE KINASE; PROTEIN-KINASE; APIGENIN;

D O I：

10.1021/jm1004368

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

NOX enzymes are the major contributors in many oxidative damage related diseases. Unfortunately, at present no specific NOX inhibitor is available. Here, we describe the discovery and development of novel NOX4 inhibitors. Compound libraries were tested in a cell-based assay as a primary screen, monitoring, H2O2 production. Twenty-four compounds inhibited NOX4 activity with low-micromolar IC50 values of which three were selected for further drug development.

引用

页码：6758 / 6762

页数：5

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