2. Academic Validation
  3. Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity

  • J Med Chem. 2012 May 10;55(9):4521-5. doi: 10.1021/jm3004009.
Won Jun Choi 1,  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
Affiliations

Affiliation

  • 1 Department of Bioinspired Science and College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
PMID: 22524616 DOI: 10.1021/jm3004009
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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