Synthesis and Biological Evaluation of Furanoallocolchicinoids

authors

• 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.

document type

abstract

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.

more information