Zebularine: a unique molecule for an epigenetically based strategy in cancer chemotherapy. The magic of its chemistry and biology |
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| Authors: | Marquez Victor E Barchi Joseph J Kelley James A Rao Kambhampati V R Agbaria Riad Ben-Kasus Tsipi Cheng Jonathan C Yoo Christine B Jones Peter A |
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| Institution: | Laboratory of Medicinal Chemistry, Center for Cancer Research, NCI at Frederick, NIH, Frederick, MD 21702, USA. marquezv@dc37a.nci.nih.gov |
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| Abstract: | 1-(beta-D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine) is structurally 4-deamino cytidine. The increased electrophilic character of this simple aglycon endows the molecule with unique chemical and biological properties, making zebularine a versatile starting material for the synthesis of complex nucleosides and an effective inhibitor of cytidine deaminase and DNA cytosine methyltransferase. Zebularine is a stable, antitumor agent that preferentially targets cancer cells and shows activity both in vitro and in experimental animals, even after oral administration. |
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