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Synthesis and biological evaluation of new tetrahydro-β-carbolines as inhibitors of the mitotic kinesin Eg5

2005; Elsevier BV; Volume: 13; Issue: 22 Linguagem: Inglês

10.1016/j.bmc.2005.06.027

1464-3391

Nils Sunder‐Plassmann, Vasiliki Sarli, Michael Gärtner, Mathias Utz, Jeanette Seiler, Stefan Huemmer, Thomas U. Mayer, Thomas Surrey, Athanassios Giannis,

14-3-3 protein interactions

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.