Synthesis and Biological Evaluation of Furanoallocolchicinoids


  • Voitovich Yuliya
  • Shegravina Ekaterina
  • Sitnikov Nikolay
  • Faerman Vladimir
  • Fokin Valery
  • Schmalz Hans-Gunther
  • Combes Sébastien
  • Allegro Diane
  • Barbier Pascale
  • Beletskaya Irina
  • Svirshchevskaya Elena
  • Fedorov Alexey Yu
  • Fedorov Alexey Yu.


A series of conformationally flexible furan-derived allocolchicinoids was prepared from commercially available colchicine in good to excellent yields using a three-step reaction sequence. Cytotoxicity studies indicated the potent activity of two compounds against human epithelial and lymphoid cell lines (AsPC-1, HEK293, and Jurkat) as well as against Wnt-1 related murine epithelial cell line W1308. The results of in vitro experiments demonstrated that the major effect of these compounds was the induction of cell cycle arrest in the G2/M phase as a direct consequence of effective tubulin binding. In vivo testing of the most potent furanoallocolchicinoid 10c using C57BL/6 mice inoculated with Wnt-1 tumor cells indicated significant inhibition of the tumor growth.

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