6533b823fe1ef96bd127f4d5

RESEARCH PRODUCT

ChemInform Abstract: The Synthesis and Effect of Fluorinated Chalcone Derivatives on Nitric Oxide Production.

M.luisa FerrándizJose N. DominguezJavier RojasMiguel Payá

subject

chemistry.chemical_classificationChalconebiologyChemistryTrimethoxychalconeGeneral MedicineCombinatorial chemistryEnzyme assayNitric oxidechemistry.chemical_compoundEnzymebiology.proteinPotencyNo production

description

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.

https://doi.org/10.1002/chin.200243112