Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity

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• 作者：Won Jun Choi ; Hwa-Jin Chung ; Girish Chandra ; Varughese Alexander ; Long Xuan Zhao ; Hyuk Woo Lee ; Akshata Nayak ; Mahesh S. Majik ; Hea Ok Kim ; Jin-Hee Kim ; Young B. Lee ; Chang H. Ahn ; Sang Kook Lee ; Lak Shin Jeong
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：May 10, 2012
• 年：2012
• 卷：55
• 期：9
• 页码：4521-4525
• 全文大小：289K
• 年卷期：v.55,no.9(May 10, 2012)
• ISSN：1520-4804

文摘

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鈥?deoxycytidine derivative 5b did not show any antigrowth effects, indicating that 2鈥?hydroxyl group is essential for the biological activity.