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Synthesis and biological evaluation of paclitaxel-thiocoichicine hybrids

Author:
  • B Danieli
  • A Giardini
  • G Lesma
  • D Passarella
  • A Silvani
  • G Appendino
  • A Noncovich
  • G Fontana
  • E Bombardelli
  • Olov Sterner
Publishing year: 2004
Language: English
Pages: 327-345
Publication/Series: Chemistry and Biodiversity
Volume: 1
Issue: 2
Document type: Journal article
Publisher: Verlag Helvetica Chimica Acta

Abstract english

The bifunctional taxoid-colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.

Keywords

  • Organic Chemistry

Other

Published
  • ISSN: 1612-1872
Olov Sterner
E-mail: olov [dot] sterner [at] science [dot] lu [dot] se

Dean

Faculty of Science

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+46 70 530 66 49

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Professor

Centre for Analysis and Synthesis

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