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The synthesis and effect of fluorinated chalcone derivatives on nitric oxide production
Javier Rojas1, Miguel Payá, José N Dominguez
1Departamento de Farmacología, Universidad de Valencia, 46100 Burjasot, Spain.
Bioorganic & Medicinal Chemistry Letters
|July 13, 2002
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) 30nM). These effects were not the consequence of a direct inhibitory action on enzyme activity but the inhibition of enzyme expression.