XB-ART-1528
Bioorg Med Chem
2005 Nov 15;1322:6094-111. doi: 10.1016/j.bmc.2005.06.027.
Show Gene links
Show Anatomy links
Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5.
???displayArticle.abstract???
The mitotic kinesin Eg5 (or KSP) is a crucial player in the development and function of the mitotic spindle. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering with other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, we report the synthesis and biological evaluation of a small library of molecules based on the structure of the known Eg5 inhibitor HR22C16. One of these derivatives (compound trans-24) proved to be a potent and specific Eg5 inhibitor.
???displayArticle.pubmedLink??? 16084101
???displayArticle.link??? Bioorg Med Chem
Species referenced: Xenopus
Genes referenced: kif11