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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Synthesis and biological evaluation of a beauveriolide analogue library.

Synthesis of beauveriolide III (1b), which is an inhibitor of lipid droplet accumulation in macrophages, was achieved by solid-phase assembly of linear depsipeptide using a 2-chlorotrityl linker followed by solution-phase cyclization. On the basis of this strategy, a combinatorial library of beauveriolide analogues was carried out by radio frequency-encoded combinatorial chemistry. After automated purification using preparative reversed-phase HPLC, the library was tested for inhibitory activity of CE synthesis in macrophages to determine structure-activity relationships of beauveriolides. Among them, we found that diphenyl derivative 7{9,1} is 10 times more potent than 1b.[1]


  1. Synthesis and biological evaluation of a beauveriolide analogue library. Nagai, K., Doi, T., Sekiguchi, T., Namatame, I., Sunazuka, T., Tomoda, H., Omura, S., Takahashi, T. Journal of combinatorial chemistry. (2006) [Pubmed]
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