Potent Kv1. 3 inhibitors from correolide—modification of the C18 position

J Bao, S Miao, F Kayser, AJ Kotliar, RK Baker…

文献索引：Bao, Jianming; Miao, Shouwu; Kayser, Frank; Kotliar, Andrew J.; Baker, Robert K.; Doss, George A.; Felix, John P.; Bugianesi, Randal M.; Slaughter, Robert S.; Kaczorowski, Gregory J.; Garcia, Maria L.; Ha, Sookhee N.; Castonguay, Laurie; Koo, Gloria C.; Shah, Kashmira; Springer, Marty S.; Staruch, Mary Jo; Parsons, William H.; Rupprecht, Kathleen M. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 2 p. 447 - 451

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被引用次数: 17

摘要

Kv1. 3, the voltage-gated potassium channel in human T cells, represents a new target for treating immunosuppression and autoimmune diseases. Correolide (1), a pentacyclic natural product, is a potent and selective Kv1. 3 channel blocker. Simplification of correolide via removal of its E-ring generates enone 4, whose modification produced a new series of tetracyclic Kv1. 3 blockers. The structure–activity relationship for this class of compounds ...