Total synthesis of azumamide A and azumamide E, evaluation as histone deacetylase inhibitors, and design of a more potent analogue |
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Authors: | Wen Shijun Carey Krystle L Nakao Yoichi Fusetani Nobuhiro Packham Graham Ganesan A |
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Institution: | School of Chemistry, University of Southampton, Southampton SO17 1BJ, United Kingdom. |
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Abstract: | The unprecedented diastereoselective Mannich reaction of a Z-allylsulfoximine was a key step in the total synthesis of the marine natural products azumamide A and E, and an unnatural analogue. Their relative potency as histone deacetylase inhibitors was evaluated and found to correlate with predicted zinc-binding affinity. reaction: see text] |
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