New chemical tools for investigating human mitotic kinesin Eg5

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

Index: 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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Citation Number: 69

Abstract

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 ...