223651-36-3Relevant articles and documents
Potent Kv1.3 inhibitors from correolide - Modification of the C18 position
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.
, p. 447 - 451 (2007/10/03)
Correolide (1) was converted to a new series of tetracyclic Kv1.3 blockers 2. SAR for this class of compounds in two functional assays, Rb_Kv and human T cell proliferation, is presented herein. 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 in two functional assays, Rb_Kv and human T cell proliferation, is presented herein. The most potent analog 43 is 15-fold more potent than correolide as inhibitor of human T cell proliferation.
Tetracyclic triterpene derivatives with immunosuppressant activity
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, (2008/06/13)
The compounds of Formula I are useful as immunosuppressive agents.
