| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367747 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
Abstract
The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared with rapamycin.
Graphical abstractThe synthesis and biological activities of highly efficacious rapamycin analogs 3 and 6 in various autoimmune disease models are reported. A shorter plasma half-life of 3 and 6, compared to rapamycin, was measured in rats, and a reduced t1/2 of 3 versus rapamycin was verified in patients.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Authors
Rolf Wagner, Karl W. Mollison, Luping Liu, Cynthia L. Henry, Teresa A. Rosenberg, Nwe Bamaung, Noah Tu, Paul E. Wiedeman, Yatsun Or, Jay R. Luly, Benjamin C. Lane, James Trevillyan, Yung-Wu Chen, Thomas Fey, Gin Hsieh, Kennan Marsh, Merrill Nuss,