Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

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

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

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.

Original languageEnglish
Pages (from-to)4521-4525
Number of pages5
JournalJournal of Medicinal Chemistry
Volume55
Issue number9
DOIs
StatePublished - 10 May 2012

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