Development and Biological Evaluation of Potent and Specific Inhibitors of Mitotic Kinesin Eg5

Abstract

Monastrol was the first specific but moderate inhibitor of the mitotic kinesin Eg5 to be identified. It proved to be useful for studies of cell division and is thought to have anticancer potential. We have synthesized a small chemical library of monastrol analogues and tested them for Eg5 inhibition in vitro and for arresting mitosis of cultured cells. We found that dimethylenastron (1) is more than 100-times more potent than monastrol in both cases. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2268/2005/z500005_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.