Publication | Closed Access
Discovery of Aryltrifluoroborates as Potent Sodium/Iodide Symporter (NIS) Inhibitors
10
Citations
12
References
2008
Year
Combinatorial ChemistryMolecular PharmacologyMedicinal ChemistryBiochemistrySodium/iodide SymporterNatural SciencesMedicineFluorous SynthesisRadiopharmaceutical TherapyStructure-based DesignPotent Sodium/iodide SymporterChemistryBf3− IonPharmacologyPharmaceutical ChemistrySmall MoleculesDrug Discovery
The structure-based design of sodium/iodide symporter (NIS) inhibitors identified new active compounds. The organotrifluoroborate shown was found to inhibit iodide uptake with an IC50 value of 0.4 μM on rat-derived thyroid cells. The biological activity is rationalized by the presence of the BF3− ion as a minimal binding motif for substrate recognition at the iodide binding site.
| Year | Citations | |
|---|---|---|
Page 1
Page 1