Synthesis of the cyclic nonapeptide of chlorofusin using a convergent [3+3+3]-fragment coupling strategy |
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| Authors: | Yan-Li Wang Wen-Jian Qian Yue Zhang |
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| Institution: | a State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China
b Department of Chemistry and Pharmaceutical Engineering, Hebei University of Technology and Science, 70 East Yuhua Road, Shijiazhuang, Hebei 050018, China |
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| Abstract: | A 3+3+3]-fragment coupling strategy was successfully applied in the synthesis of the nonacyclopeptide of chlorofusin, a potent natural antagonist against p53-MDM2 interactions. The accomplished convergent synthesis includes parallel syntheses of three tripeptides and their sequential assembly, and macrocyclization of the linear precursor to the required 27-membered nonacyclopeptide. |
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