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Curr Top Med Chem. 2017;17(26):2935-2956. doi: 10.2174/1568026617666170821124947.

Update on COX-2 Selective Inhibitors: Chemical Classification, Side Effects and their Use in Cancers and Neuronal Diseases.

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Equipe de Chimie Moleculaire, Laboratoire de Chimie Moleculaire, Genie des Procedes Chimiques et Energetiques, EA7341, Conservatoire National des Arts et Metiers, 2 rue Conte, 75003 Paris. France.
Laboratoire Genomique Bioinformatique et Applications, EA 4627, Conservatoire National des Arts et Metiers, 292 rue Saint Martin, 75003 Paris. France.


Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and providing a new target for the development of COX-2-selective drugs without gastrointestinal side-effects. Keeping in view the importance of this pharmacological class, several literature reports have underlined the impact of these antiinflammatory compounds in therapeutics. The present review considers the most recently published literature concerning COX-2 inhibitors until 2016. Through a wide chemical classification, the last developments concerning this therapeutic family by highlighting structure-activity relationships insights and mechanisms are presented. A summary of the principal adverse effects observed and an overview of the new potential therapeutic indications for COX-2 inhibitors are also reported.


COX-1/COX-2 inhibition; COX-2 inhibitors; Cyclooxygenase; Inflammation; Non-steroidal anti-inflammatory Drugs; Structure–activity relationship

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