Biological Evaluation and Molecular Docking Study of 3-(4-Sulfamoylphenyl)-4-phenyl-1H-pyrrole-2,5-dione as GOX-2 Inhibitor

摘要

Cyclooxygenase (COX) is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Three COX isoenzymes are known: COX-1, COX-2, and COX-3 which is a splice variant of COX-1. COX-1 is considered a constitutive enzyme, being found in most mammalian cells. On the other hand, COX-2, undetectable in normal tissues, and induced during inflammation, hypoxia and Wnt-signalling, is present in many cancers. Classical non-steroidal anti'-inflammatory drugs (NSAIDs) such as aspirin block both COX-1 and COX-2. When the COX-1 is inhibited, inflammation is reduced, but the protection of the lining of the stomach is also lost. This can cause stomach upset as well as ulceration and bleeding from the stomach and even the intestines.