Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594139 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
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 â¼0.5 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.
Keywords
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Chemistry
Organic Chemistry
Authors
Chalet Tan, Rita G. de Noronha, Narra S. Devi, Adnan A. Jabbar, Stefan Kaluz, Yuan Liu, Suazette Reid Mooring, K.C. Nicolaou, Binghe Wang, Erwin G. Van Meir,