Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents

Cancer is considered as one of the most serious health problems. Despite the presence of many effective chemotherapeutic agents, their severe side effects together with the appearance of mutant tumors limit the use of these drugs and increase the need for new anticancer agents. Eg5 represents an attractive target for medicinal chemists since Eg5 is overexpressed in many proliferative tissues while almost no Eg5 is detected in nonproliferative tissues. Many Eg5 inhibitors displayed potent anticancer activity against some of the mutant tumors with limited side effects. The present review provides an overview about the progress in the discovery of Eg5 inhibitors especially from 2009 to 2012 as well as the clinical trials conducted on some of these inhibitors.

Graphical abstractThe present review provides an overview about the progress in the discovery of Eg5 inhibitors and their clinical trials especially from 2009 to 2012.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Eg5 is an attractive target for medicinal chemists. ► Eg5 is overexpressed in many proliferative tissues. ► Eg5 inhibitors displayed potent anticancer activity against mutant tumors. ► The present review provides overview about the progress in the discovery of Eg5 inhibitors.