Unsaturated fluoroketonucleosides as anticancer agents: the synthesis and biological activity of 5-fluoro-1-(3,4-di-deoxy-3-fluoro-6-O-trityl-beta-d-glycero-hex-3-eno-pyranos-2- ulosyl) uracil |
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Authors: | Egron M J Dorange B I Antonakis K Herscovici J Ollapally A P |
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Institution: | Ecole Nationale Supzrieure de Chimie, CNRS-UMR 7001, Paris, France. |
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Abstract: | Direct oxidation of 5-fluoro-1-(4-O-acetyl-3-deoxy-3-fluoro-6-O-trityl-beta-D-glucopyranosyl) uracil 9 led to the title compound 10 after a beta-elimination reaction. The formation of the hydrate of ketone 10 due to the highly electronegative fluorine atom in the a position to the carbonyl group, prompted us to carry out a comparative study of different methods of oxidation and to define the best strategy for the synthesis of such molecules. Results of in vitro and in vivo biological evaluations are reported. |
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