Publikation:

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

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2005

Autor:innen

Sunder-Plassmann, Nils
Sarli, Vasiliki
Gartner, Michael
Utz, Mathias
Seiler, Jeanette
Huemmer, Stefan
Surrey, Thomas
Giannis, Athanassios

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http://nbn-resolving.de/urn:nbn:de:bsz:352-140474
DOI (zitierfähiger Link)
https://doi.org/10.1016/j.bmc.2005.06.027
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Biologie: Publikationen
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Published

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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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ISO 690SUNDER-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.2005.06.027
BibTex
@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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