Chemical and Pharmaceutical Bulletin · 2005 · 18 citations · 9 references
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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Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami et al. · Journal of Medicinal Chemistry · 2000 · 114 citations · Full text
Combinatorial Chemistry, Medicinal Chemistry, Pharmacological Characterization +15