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Journal Articles Journal of Medicinal Chemistry Year : 2014

Synthesis and Biological Evaluation of Furanoallocolchicinoids


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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hal-01744566 , version 1 (27-03-2018)



Yuliya Voitovich, Ekaterina Shegravina, Nikolay Sitnikov, Vladimir Faerman, Valery Fokin, et al.. Synthesis and Biological Evaluation of Furanoallocolchicinoids. Journal of Medicinal Chemistry, 2014, 58 (2), pp.692 - 704. ⟨10.1021/jm501678w⟩. ⟨hal-01744566⟩
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