Publikation: Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5
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Datum
2005
Autor:innen
Sunder-Plassmann, Nils
Sarli, Vasiliki
Gartner, Michael
Utz, Mathias
Seiler, Jeanette
Huemmer, Stefan
Surrey, Thomas
Giannis, Athanassios
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Bioorganic & Medicinal Chemistry. 2005, 13(22), pp. 6094-6111. ISSN 0968-0896. Available under: doi: 10.1016/j.bmc.2005.06.027
Zusammenfassung
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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Fachgebiet (DDC)
570 Biowissenschaften, Biologie
Schlagwörter
small molecule, Eg5, Kinesin
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SUNDER-PLASSMANN, Nils, Vasiliki SARLI, Michael GARTNER, Mathias UTZ, Jeanette SEILER, Stefan HUEMMER, Thomas U. 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. 2005, 13(22), pp. 6094-6111. ISSN 0968-0896. Available under: doi: 10.1016/j.bmc.2005.06.027BibTex
@article{SunderPlassmann2005-11-15Synth-14047, year={2005}, doi={10.1016/j.bmc.2005.06.027}, title={Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5}, 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 U. and Surrey, Thomas and Giannis, Athanassios} }
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