Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity |
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Authors: | Choi Won Jun Chung Hwa-Jin Chandra Girish Alexander Varughese Zhao Long Xuan Lee Hyuk Woo Nayak Akshata Majik Mahesh S Kim Hea Ok Kim Jin-Hee Lee Young B Ahn Chang H Lee Sang Kook Jeong Lak Shin |
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Affiliation: | Department of Bioinspired Science and College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea. |
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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 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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