期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 2, 页码 692-704出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm501678w
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资金
- Russian Foundation for Basic Research [14-03-91342]
- Ministry of Education and Science of The Russian Federation [4.619.2014/K, 02.B.49.21.0003]
- German Science Foundation (DFG) [Schm 857/18-1]
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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