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J Med Chem. 2012 May 10;55(9):4521-5. doi: 10.1021/jm3004009. Epub 2012 May 1.

Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity.

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1
Department of Bioinspired Science and College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.

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.

PMID:
22524616
DOI:
10.1021/jm3004009
[Indexed for MEDLINE]

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