Structure and activity relationships of tartrate-based TACE inhibitors

D Li, J Popovici-Muller, DB Belanger, J Caldwell…

文献索引：Li, Dansu; Popovici-Muller, Janeta; Belanger, David B.; Caldwell, John; Dai, Chaoyang; David, Maria; Girijavallabhan, Vinay M.; Lavey, Brian J.; Lee, Joe F.; Liu, Zhidan; Mazzola, Rob; Rizvi, Razia; Rosner, Kristin E.; Shankar, Bandarpalle; Spitler, Jim; Ting, Pauline C.; Vaccaro, Henry; Yu, Wensheng; Zhou, Guowei; Zhu, Zhaoning; Niu, Xiaoda; Sun, Jing; Guo, Zhuyan; Orth, Peter; Chen, Shiying; Kozlowski, Joseph A.; Lundell, Daniel J.; Madison, Vincent; McKittrick, Brian; Piwinski, John J.; Shih, Neng-Yang; Shipps Jr., Gerald W.; Siddiqui, M. Arshad; Strickland, Corey O. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 16 p. 4812 - 4815

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被引用次数: 7

摘要

Tumor necrosis factor-α (TNF-α) is a proinflammatory cytokine that plays a central role in several autoimmune disorders such as rheumatoid arthritis (RA), Crohn's disease, and psoriasis. 1 The current success of anti-TNF-α biologics such as Enbrel®, Remicade®, and Humira® in the treatment of RA has increased interest in discovering an orally active small molecule inhibitor to modulate the level of TNF-α. ... Recently, we disclosed a novel series of tartrate diamide TACE ...