Cyclooxygenase-2 (COX-2) is an inducible enzyme that has an integral role in inflammation and contributes to the progression of its associated diseases such as cancer.  Consequently, COX-2 has been identified as a target enzyme for the design of novel compounds aimed at treating certain cancers.  Flavonoids, a class of polyphenol natural products found in fruits, vegetables, and many plant species, have shown great promise as potential anti-cancer agents as they exhibit anti-inflammatory, antioxidant, and COX-2 inhibitory activity.  Despite their biological potential, the use of flavonoids as therapeutic agents is limited by several factors, such as poor bioavailability and absorption.  To overcome these limitations, recent structure-activity studies show that masking flavonoid hydroxyls as ether groups improve their pharmacological activities. As such, a series of methylated flavonoid derivatives were synthesized, characterized and evaluated for their COX-2 inhibitory activity. <br/>

Synthesis, characterization and biological testing of methylated flavonoid derivatives as potential cyclooxygenase-2 inhibitors

255th National Meeting (2018)

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