Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(Aryloyl) phenyl methyl sulfones

Y Harrak, G Casula, J Basset, G Rosell…

文献索引：Harrak, Youssef; Casula, Giovanni; Basset, Joan; Rosell, Gloria; Plescia, Salvatore; Raffa, Demetrio; Cusimano, Maria Grazia; Pouplana, Ramon; Pujol, Maria Dolors Journal of Medicinal Chemistry, 2010 , vol. 53, # 18 p. 6560 - 6571

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被引用次数: 47

摘要

Following our previous research on anti-inflammatory drugs (NSAIDs), we report on the design and synthesis of 4-(aryloyl) phenyl methyl sulfones. These substances were characterized for their capacity to inhibit cyclooxygenase (COX-1 and COX-2) isoenzymes. Molecular modeling studies showed that the methylsulfone group of these compounds was inserted deep in the pocket of the human COX-2 binding site, in an orientation that ...