Zebularine: a unique molecule for an epigenetically based strategy in cancer chemotherapy

  • Ann N Y Acad Sci. 2005 Nov:1058:246-54. doi: 10.1196/annals.1359.037.
Victor E Marquez  1 ,  James A Kelley ,  Riad Agbaria ,  Tisipi Ben-Kasus ,  Jonathan C Cheng ,  Christine B Yoo ,  Peter A Jones
Affiliations
  • 1. Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute at Frederick, NIH, Frederick, Maryland 21702, USA. [email protected]
PMID: 16394141 DOI: 10.1196/annals.1359.037
Abstract

1-(Beta-d-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine) corresponds structurally to Cytidine minus the exocyclic 4-amino group. The increased electrophilic character of its simple aglycon endows the molecule with unique biologic properties as a potent inhibitor of both Cytidine deaminase and DNA Cytosine methyltransferase. The latter activity makes zebularine a promising antitumor agent that is hydrolytically stable, preferentially targets Cancer cells, and shows activity both in vitro and in experimental Animals, even after oral administration.

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