Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4

Hall, J.J. et al. (2008) Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4. Bioorganic and Medicinal Chemistry Letters, 18(18), pp. 5146-5149. (doi: 10.1016/j.bmcl.2008.07.070)

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Publisher's URL: http://dx.doi.org/10.1016/j.bmcl.2008.07.070

Abstract

A new trifluorinated amino-combretastatin analogue, (Z)-2-(4′-methoxy-3′-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC<sub>50</sub> = 2.9 μM), and cytotoxic against selected human cancer cell lines. This new lead compound is among the most active from a group of related structural modifications.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Gaddale Devanna, Dr Kishore Kumar
Authors: Hall, J.J., Sriram, M., Strecker, T.E., Tidmore, J.K., Jelinek, C.J., Kumar, G.D.K., Hadimani, M.B., Pettit, G.R., Chaplin, D.J., Trawick, M.L., and Pinney, K.G.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Bioorganic and Medicinal Chemistry Letters
ISSN:0960-894X
ISSN (Online):1464-3405

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