Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

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 5a 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 5b did not show any antigrowth effects, indicating that 2′-hydroxyl group is essential for the biological activity. © 2012 American Chemical Society.