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Biological Evaluation of 2-Aryl-2-fluoropropionic Acids as Possible Platforms for New Medicinal Agents
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References
2005
Year
Pharmaceutical ScienceBioorganic ChemistryPharmacotherapy2-Aryl-2-fluoropropionic AcidsAntimicrobial ChemotherapyPharmaceutical ChemistryMedicinal ChemistryBiological EvaluationAnti-cancer AgentRetained Inhibitory ActivityCox-1/cox-2 InhibitionsBiochemistryPharmacological AgentNew Medicinal AgentsAntimicrobial CompoundDrug DevelopmentPharmacologyAnti-inflammatoryNatural SciencesMedicineLower Inhibitory ActivityDrug Discovery
We investigated the cyclooxygenase (COX) inhibitory and anticancer activities of 2-aryl-2-fluoropropionic acids 1a-e. These fluorinated compounds showed lower inhibitory activity toward COX-1 than the corresponding non-fluorinated compounds 2a-e with retained inhibitory activity against COX-2 resulting in modification of the balance of COX-1/COX-2 inhibitions, and they showed little anticancer activity. Interesting differences of the activities between (S)- and (R)-enantiomers were observed in some cases.
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