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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

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SUNDER-PLASSMANN, Nils, Vasiliki SARLI, Michael GARTNER, Mathias UTZ, Jeanette SEILER, Stefan HUEMMER, Thomas MAYER, Thomas SURREY, Athanassios GIANNIS, 2005. Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5. In: Bioorganic & Medicinal Chemistry. 13(22), pp. 6094-6111. ISSN 0968-0896. Available under: doi: 10.1016/j.bmc.2005.06.027

@article{SunderPlassmann2005-11-15Synth-14047, title={Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5}, year={2005}, doi={10.1016/j.bmc.2005.06.027}, number={22}, volume={13}, issn={0968-0896}, journal={Bioorganic & Medicinal Chemistry}, pages={6094--6111}, author={Sunder-Plassmann, Nils and Sarli, Vasiliki and Gartner, Michael and Utz, Mathias and Seiler, Jeanette and Huemmer, Stefan and Mayer, Thomas and Surrey, Thomas and Giannis, Athanassios} }

Seiler, Jeanette 2011-12-14T10:22:08Z deposit-license Sarli, Vasiliki Surrey, Thomas Seiler, Jeanette Surrey, Thomas Publ. in: Bioorganic & Medicinal Chemistry ; 13 (2005), 22. - S. 6094-6111 Utz, Mathias 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. Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5 Sunder-Plassmann, Nils Utz, Mathias Huemmer, Stefan Sarli, Vasiliki Giannis, Athanassios eng Gartner, Michael Mayer, Thomas Sunder-Plassmann, Nils Huemmer, Stefan 2005-11-15 2011-12-14T10:22:08Z Gartner, Michael Giannis, Athanassios Mayer, Thomas

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