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    Synthesis and in vitro evaluation of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives as thymidine phosphorylase inhibitors

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    Fulltext not available
    Authors
    Bera, H.
    Dolzhenko, Anton
    Sun, L.
    Dutta Gupta, S.
    Chui, W.
    Date
    2013
    Type
    Journal Article
    
    Metadata
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    Citation
    Bera, H. and Dolzhenko, A. and Sun, L. and Dutta Gupta, S. and Chui, W. 2013. Synthesis and in vitro evaluation of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives as thymidine phosphorylase inhibitors. Chemical Biology and Drug Design. 82 (3): pp. 351-360.
    Source Title
    Chemical Biology and Drug Design
    DOI
    10.1111/cbdd.12171
    ISSN
    1747-0277
    School
    School of Pharmacy
    URI
    http://hdl.handle.net/20.500.11937/33573
    Collection
    • Curtin Research Publications
    Abstract

    In our lead finding program, a series of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives were synthesized, and their in vitro thymidine phosphorylase inhibitory potential was explored. Among the different derivatives, compounds having keto group (C = O) at C7 and thioketo group (C = S) at C5 positions showed varying degrees of TP inhibitory activity comparable with positive control, 7-deazaxanthine (7-DX, 2) (IC50 value = 42.63 µm). Enzyme inhibition kinetics study suggested that compound IVn behaved as a mixed-type inhibitor of the enzyme with respect to thymidine (dThd) as a variable substrate. Compound IVn was also found to inhibit PMA-induced MMP-9 expression in MDA-MB-231 cells at sublethal concentrations. Computational docking study was performed to illustrate the enzyme inhibition kinetics and to explore the ligand-enzyme interactions. © 2013 John Wiley & Sons A/S.

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