Solid-phase synthesis of a pepticinnamin E library |
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| Authors: | Thutewohl Michael Waldmann Herbert |
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| Affiliation: | 1. The Lipid Research Laboratory, Rappaport Faculty of Medicine, Technion–Israel Institute of Technology, Haifa, Israel;2. Department of Internal Medicine E, Rambam Health Care Campus, Haifa, Israel;3. Laboratory of Clinical Biochemistry, Rambam Health Care Campus, Haifa, Israel |
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| Abstract: | Pepticinnamin E is a naturally occurring bisubstrate inhibitor of farnesyltransferase. Based on the structure of the natural product, a compound library was synthesized by variation of eight structural parameters. Following three different routes, a total of 51 analogues was synthesized on the polymeric support in 6-11-step parallel syntheses. Overall yields ranged from 3 to 63%, and the compounds were obtained with >90% purity. |
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