Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 9, Pages 4521-4525Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm3004009
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Funding
- WCU [R31-2008-000-10010-0]
- National Research Foundation (NRF)
- Seoul RBD Program [ST100039]
- GRRC of Gyeonggi province [GRRC-DONGGUK2011-B02]
- Ewha Womans University [2011]
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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.
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