Synthesis and antitumor activities of novel 5′-deoxy-5-fluorocytidine derivatives

Paper

Synthesis and antitumor activities of novel 5′-deoxy-5-fluorocytidine derivatives

Published 2007 · Wu Guang

Chinese Journal of Medicinal Chemistry

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Abstract

Aim To design and synthesize 5′-deoxy-5-fluorocytidine derivatives as antitumor drugs.Methods A series of 5′-deoxy-5-fluorocytidine alkylamine,alkoxyl and amidine derivatives were synthesized by displacement of triazole group at C-4 of 1-(2′,3′-O-diacetyl-5′-deoxy-β-D-ribofuranosyl)-4-(1,2,4-triazol-1-yl)-5-fluoropyrimidin-2-(1H)-one,which was obtained conveniently by condensation between 2′,3′-O-diacetyl-5′-deoxy-5-fluorocytidine and 1,2,4-triazole in the presence of POCl3.Results Fifteen new compounds were prepared,all of the products were confirmed by 1H-NMR,FAB-MS,and elemental analysis.Conclusion Antitumor activity results indicated that some of the title compounds had similar inhibitory effect on the lung cancer cell,breast cancer cell,liver cancer cell,and colon cancer cell as capecitabine did.

In Vitro Study

Study Snapshot

Novel 5′-deoxy-5-fluorocytidine derivatives show potential as antitumor drugs with similar inhibitory effects on lung, breast, liver, and colon cancer cells as capecitabine.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Synthesis and antitumor activities of novel 5′-deoxy-5-fluorocytidine derivatives

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