Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl) phenyl] methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors

…, L Ma, W Huang, X Yu, Y Zhang, H Ji, J Tian

文献索引：Lai, Yisheng; Ma, Lin; Huang, Wenxing; Yu, Xing; Zhang, Yihua; Ji, Hui; Tian, Jide Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7349 - 7353

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被引用次数: 29

摘要

Fourteen new 3-[4-(amino/methylsulfonyl) phenyl] methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5- LOX with IC50 in the range of 0.10–9.87 μM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (IC50= 0.10–0.56 μM). More importantly, 10f and several other compounds had comparable or stronger anti-inflammatory and analgesic activities, ...