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Synthesis and biological evaluation of paclitaxel-thiocoichicine hybrids

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Author

  • B Danieli
  • A Giardini
  • G Lesma
  • D Passarella
  • A Silvani
  • G Appendino
  • A Noncovich
  • G Fontana
  • E Bombardelli
  • Olov Sterner

Summary, in 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.

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

Topic

  • Organic Chemistry

Status

Published

ISBN/ISSN/Other

  • ISSN: 1612-1872