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• W2029968342 abstract "Solid tumors generally grow under hypoxic conditions, a pathophysiological change, which activates the expression of genes responsible for malignant, aggressive, and treatment-refractory properties. Hypoxia inducible factor (HIF) is the chief transcription factor regulating hypoxia-driven gene expression. Therefore, the HIF pathway has become a critical target for cancer therapeutics development. We screened a privileged library of about 10,000 natural-product-like compounds using a cell-based assay for HIF-dependent transcriptional activity and identified several arylsulfonamide HIF pathway inhibitors. Among these compounds, the most potent ones showed an IC50 of ∼0.5 μM in the hypoxia-responsive element (HRE)-luciferase reporter system. Further studies are needed to fully elucidate the mechanism of action of this class of compounds and their structure–activity relationship." @default.
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• W2029968342 date "2011-09-01" @default.
• W2029968342 modified "2023-10-11" @default.
• W2029968342 title "Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors" @default.
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• W2029968342 doi "https://doi.org/10.1016/j.bmcl.2011.06.099" @default.
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