New chemical tools for investigating human mitotic kinesin Eg5

…, S DeBonis, B Thiede, DA Skoufias, F Kozielski…

文献索引：Klein, Emmanuel; DeBonis, Salvatore; Thiede, Bernd; Skoufias, Dimitrios A.; Kozielski, Frank; Lebeau, Luc Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 19 p. 6474 - 6488

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被引用次数: 69

摘要

We have designed and synthesized a series of monastrol derivatives, an allosteric inhibitor of Eg5, a motor protein responsible for the formation and maintenance of the bipolar spindle in mitotic cells. Sterically demanding structural modifications have been introduced on the skeleton of the parent drug either via a multicomponent Biginelli reaction or a stepwise modification of monastrol. The ability of these compounds to inhibit Eg5 activity has been ...