Fluorocyclopentenyl-cytosine
with Broad Spectrum and
Potent Antitumor Activity
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Abstract
On the basis of the potent biological activity of cyclopentenyl-pyrimidines,
fluorocyclopentenyl-pyrimidines were designed and synthesized from d-ribose. Among these, the cytosine derivative <b>5a</b> showed highly potent antigrowth effects in a broad range of tumor
cell lines and very potent antitumor activity in a nude mouse tumor
xenograft model implanted with A549 human lung cancer cells. However,
its 2′-deoxycytidine derivative <b>5b</b> did not show
any antigrowth effects, indicating that 2′-hydroxyl group is
essential for the biological activity