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    Synthesis, in vitro evaluation of thymidine phosphorylase inhibitory activity, and in silico study of 1,3,5-triazin-2,4-dione and its fused analogues

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    Authors
    Bera, H.
    Chui, W.
    Gupta, S.
    Dolzhenko, Anton
    Sun, L.
    Date
    2013
    Type
    Journal Article
    
    Metadata
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    Citation
    Bera, H. and Chui, W. and Gupta, S. and Dolzhenko, A. and Sun, L. 2013. Synthesis, in vitro evaluation of thymidine phosphorylase inhibitory activity, and in silico study of 1,3,5-triazin-2,4-dione and its fused analogues. Medicinal Chemistry Research. 22 (12): pp. 6010-6021.
    Source Title
    Medicinal Chemistry Research
    DOI
    10.1007/s00044-013-0589-1
    ISSN
    1054-2523
    School
    School of Pharmacy
    URI
    http://hdl.handle.net/20.500.11937/29884
    Collection
    • Curtin Research Publications
    Abstract

    Based on structural similarities with the reference compounds, a series of 1,3,5-triazin-2,4-dione and their fused analogues was designed, synthesized and their in vitro thymidine phosphorylase inhibitory potential was evaluated. The monocyclic analogues were found to be inactive. Among the different fused derivatives synthesized, compounds having keto group (C=O) at C7/C4 and thioketo group (C=S) at C5/C2 position showed TP inhibitory activity comparable to positive control, 7-deazaxanthine (7-DX) (IC50 value = 42.63 µM). Molecular docking of the target compounds into the enzyme thymidine phosphorylase was performed to illustrate the important structural information on the plausible ligand-enzyme-binding interactions. © 2013 Springer Science+Business Media New York.

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