Cyclooxygenase (Cox) is a key enzyme in the biosynthesis of prostaglandins and, as such, is the target of non-steroidal anti-inflammatory drugs (NSAIDs). Two isoforms exist, being expressed constitutively (Cox-1), or inducibly in response to inflammatory mediators (Cox-2). Currently available NSAIDs inhibit both isoforms somewhat equipotently but selective Cox-2 inhibition may eliminate unwante...

The transformed monocyte/macrophage cell line J774.2 undergoes apoptosis when treated for 48 h with competitive inhibitors of cyclooxygenase (COX) isoenzymes 1 and 2. Many of these nonsteroid antiinflammatory drugs (NSAIDs), but in particular diclofenac, induce during this time period a COX activity that coincides with a robust induction of COX-2 protein. Induction of this activity requires hig...

Aspirin eugenol ester (AEE) is a promising drug candidate, which is used for the treatment of inflammation, pain and fever and the prevention of cardiovascular diseases. This study focuses on the effect of AEE on five proteins which are related to inflammation and thrombosis, including cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), C-reactive protein (CRP), prothrombin (FII) and arachidona...

Non-melanoma skin cancers (NMSCs) are among the most common human malignancies. Current methods for their prevention include avoidance of natural and artificial sources of UV radiation and using photoprotective clothing and sunscreens. However, these methods have proven to be inadequate in stemming the rise in skin cancer incidence over the past several years. There is accumulating evidence tha...

Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently used antipyretic agents that most probably exert their antifever effect by inhibiting cyclooxygenase (COX)-2. Thus, COX-2-selective drugs or null mutation of the COX-2 gene reduce or prevent fever. Acetaminophen is antipyretic and analgesic, as are NSAIDs, but it lacks the anti-inflammatory and anticoagulatory properties of these drug...

a group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a cox-2 so2me pharmacophore at the para position of the c-2 or c-4 phenyl ring, in conjunction with a c-4 or c-2 phenyl (4-h) or substituted-phenyl ring (4-f,4-cl,4-br,4-ome,4-me, 4-no2), were designed for evaluation as selective cyclooxygenase-2 (cox-2) inhibitors. these target 5-oxo-1,4,5,6,7,8 hexahydroquino...