Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity
Won Jun Choi(Ewha Womans University), Hwa‐Jin Chung(Seoul National University), Girish Chandra(Ewha Womans University), Varughese Alexander(Ewha Womans University), Long Zhao(Liaoning Normal University), Hyuk Woo Lee(Ewha Womans University), Akshata Nayak(Ewha Womans University), Mahesh S. Majik(Ewha Womans University), Hea Ok Kim(Ewha Womans University), Jin‐Hee Kim(Ewha Womans University), Young Bok Lee(Psyadon Pharmaceuticals (United States)), Chang Ho Ahn(Psyadon Pharmaceuticals (United States)), Sang Kook Lee(Seoul National University), Lak Shin Jeong(Ewha Womans University)
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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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