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    A structure-activity relationship study of 1,2,4-triazolo[1,5-a][1,3,5] triazin-5,7-dione and its 5-thioxo analogues on anti-thymidine phosphorylase and associated anti-angiogenic activities

    Access Status
    Fulltext not available
    Authors
    Bera, H.
    Tan, B.
    Sun, L.
    Dolzhenko, Anton
    Chui, W.
    Chiu, G.
    Date
    2013
    Type
    Journal Article
    
    Metadata
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    Citation
    Bera, H. and Tan, B. and Sun, L. and Dolzhenko, A. and Chui, W. and Chiu, G. 2013. A structure-activity relationship study of 1,2,4-triazolo[1,5-a][1,3,5] triazin-5,7-dione and its 5-thioxo analogues on anti-thymidine phosphorylase and associated anti-angiogenic activities. European Journal of Medicinal Chemistry. 67: pp. 325-334.
    Source Title
    European Journal of Medicinal Chemistry
    DOI
    10.1016/j.ejmech.2013.06.051
    ISSN
    0223-5234
    School
    School of Pharmacy
    URI
    http://hdl.handle.net/20.500.11937/4279
    Collection
    • Curtin Research Publications
    Abstract

    Thirty-three 1,2,4-triazolo[1,5-a][1,3,5]triazin-5,7-dione and its 5-thioxo analogues were designed and synthesized which contained different substituents at meta- and/or para-positions of 2-phenyl or 2-benzyl ring attached to the fused ring structure. The preliminary pharmacological evaluation demonstrated that the 5-thioxo analogues of 1,2,4-triazolo[1,5-a][1,3,5]triazine exhibited a varying degree of inhibitory activity towards thymidine phosphorylase, comparable or better than reference compound, 7-Deazaxanthine (7-DX, 2) (IC 50 value = 42.63 µM). Moreover, compounds 5q and 6i displayed a mixed-type of inhibitory mechanism in the presence of variable concentrations of thymidine (dThd). In addition, selected compounds were found to have a noticeable inhibitory effect on the expression of angiogenesis markers, including VEGF and MMP-9 in MDA-MB-231 breast cancer cells. © 2013 Elsevier Masson SAS. All rights reserved.

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