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Small-molecule inhibitors of NADPH oxidase 4

, : Small-molecule inhibitors of NADPH oxidase 4. Journal of Medicinal Chemistry 53(18): 6758-6762

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 IC(50) values of which three were selected for further drug development.


PMID: 20731357

DOI: 10.1021/jm1004368

Other references

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