1242078-01-8Relevant articles and documents
Design, synthesis, and biological evaluation of ketoprofen analogs as potent cyclooxygenase-2 inhibitors
Zarghi, Afshin,Ghodsi, Razieh
, p. 5855 - 5860 (2010)
A new series of ketoprofen analogs were synthesized to evaluate their biological activities as selective cyclooxygenase-2 (COX-2) inhibitors. In vitro COX-1 and COX-2 inhibition studies showed that all compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 values in the highly potent 0.057-0.085 μM range, and COX-2 selectivity indexes in the 115 to >1298.7 range. Compounds possessing azido pharmacophore group (8a and 8b) exhibited highly COX-2 inhibitory selectivity and potency even more than reference drug celecoxib. Molecular modeling studies indicated that the azido substituent can be inserted deeply into the secondary pocket of COX-2 active site for interactions with Arg513.
