6533b830fe1ef96bd12971a5
RESEARCH PRODUCT
The synthesis and effect of fluorinated chalcone derivatives on nitric oxide production
Jose N. DominguezMiguel PayáM.luisa FerrándizJavier Rojassubject
LipopolysaccharidesChalconeHydrocarbons FluorinatedClinical BiochemistryNitric Oxide Synthase Type IIPharmaceutical ScienceEtherNitric OxideBiochemistryChemical synthesisCell LineNitric oxideInhibitory Concentration 50MiceStructure-Activity Relationshipchemistry.chemical_compoundChalconeDrug DiscoveryAnimalsOrganic chemistryMolecular BiologyNitriteschemistry.chemical_classificationbiologyChemistryMacrophagesAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryHaloketoneCombinatorial chemistryEnzyme assayEnzymeEnzyme Inductionbiology.proteinMolecular MedicineNitric Oxide SynthaseEnonedescription
Abstract Dimethoxy- and trimethoxychalcone derivatives, with various patterns of fluorination, were synthesized and evaluated for their influence on nitric oxide production. Some of them, chalcones 1 , 5 , 7 , 10 , 11 and 17 , inhibited NO production with an IC 50 in the submicromolar range; 17 is especially noteworthy because of its potency (IC 50 30 nM). These effects were not the consequence of a direct inhibitory action on enzyme activity but the inhibition of enzyme expression.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2002-08-01 | Bioorganic & Medicinal Chemistry Letters |