2. Academic Validation
  3. Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5

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

  • Bioorg Med Chem. 2005 Nov 15;13(22):6094-111. doi: 10.1016/j.bmc.2005.06.027.
Nils Sunder-Plassmann 1,  Vasiliki Sarli,  Michael Gartner,  Mathias Utz,  Jeanette Seiler,  Stefan Huemmer,  Thomas U Mayer,  Thomas Surrey,  Athanassios Giannis
Affiliations

Affiliation

  • 1 University of Leipzig, Institute for Organic Chemistry, Johannisallee 29, 04103 Leipzig, Germany.
PMID: 16084101 DOI: 10.1016/j.bmc.2005.06.027
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.

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