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2 '-deoxy-N4-[2-(4-nitrophenyl)ethoxycarbonyl]-5-azacytidine: A novel inhibitor of DNA methyltransferase that requires activation by human carboxylesterase

  1. Author:
    Byun, H. M.
    Choi, S. H.
    Laird, P. W.
    Trinh, B.
    Siddiqui, M. A.
    Marquez, V. E.
    Yang, A. S.

  2. Author Address

    Byun, Hyang-Min, Choi, Si Ho, Yang, Allen S.] Univ So Calif, Kenneth Norris Jr Comprehens Canc Ctr, Div Hematol, Los Angeles, CA 90033 USA. [Laird, Peter W.; Trinh, Binh] Univ So Calif, Kenneth Norris Jr Comprehens Canc Ctr, Dept Surg, Los Angeles, CA 90033 USA. [Laird, Peter W.; Trinh, Binh] Univ So Calif, Kenneth Norris Jr Comprehens Canc Ctr, Dept Biochem & Mol Biol, Los Angeles, CA 90033 USA. [Siddiqui, Maqbool A.; Marquez, Victor E.] NCI, Ctr Canc Res, Med Chem Lab, Frederick, MD 21701 USA.
    1. Year: 2008
  2. Journal: Cancer Letters
    1. 266
    2. 2
    3. Pages: 238-248
  4. Type of Article: Article
  1. Abstract:

    2 '-Deoxy-N4-[2-(4-nitrophenyl)ethoxycarbonyl]-5-azacytidine (NPEOC-DAC), decitabine with a modification of the N4 position of the azacitidine ring can be used to inhibit DNA methyltransferase. This modification protects the azacitidine ring and can be cleaved by carboxylesterase to release decitabine. NPEOC-DAC was 23-fold less potent at low doses (<10 mu M) than decitabine at inhibiting DNA methylation, and was also associated with a 3-day delay in its effect. However, at doses >= 10 mu M NPEOC-DAC was more effective at inhibiting DNA methylation. Theses differences between decitabine and NPEOC-DAC are dependent on the cleavage of the carboxylester bond, and could be potentially exploited pharmacologically. (C) 2008 Elsevier Ireland Ltd. All rights reserved.

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External Sources

  1. PMID: 18499340

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