Natural product based inhibitors of the thioredoxin–thioredoxin reductase system
Copyright policy )Natural product based inhibitors of the thioredoxin–thioredoxin reductase system
Spiroketal naphthodecalins are readily assembled by Barton's base mediated Ullmann binaphthyl ether coupling, Dakin reactions and hypervalent iodine spirocyclization. The core structures can be further diversified by enone addition and Stille coupling reactions. Nanomolar inhibitors for the Trx/TrxR redox control system were prepared by this approach and compared to series of natural product isolates. Cytotoxicity in MCF-7 cell assays ranged from an IC50 of 1.6 to >100 microM.
- University of Pittsburgh United States
- University of Costa Rica Costa Rica
- Instituto Nacional de Biodiversidad
- National Biodiversity Institute Costa Rica
- University of Arizona United States
Natural products, Thioredoxin-Disulfide Reductase, Molecular Structure, Inhibitors, Antineoplastic Agents, Inhibitory Concentration 50, Thioredoxins, Cell Line, Tumor, Humans, Spiro Compounds, Drug Screening Assays, Antitumor, Enzyme Inhibitors, Thioredoxin, Naphthoquinones
Natural products, Thioredoxin-Disulfide Reductase, Molecular Structure, Inhibitors, Antineoplastic Agents, Inhibitory Concentration 50, Thioredoxins, Cell Line, Tumor, Humans, Spiro Compounds, Drug Screening Assays, Antitumor, Enzyme Inhibitors, Thioredoxin, Naphthoquinones
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