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dc.contributor.authorBera, H.
dc.contributor.authorDolzhenko, Anton
dc.contributor.authorSun, L.
dc.contributor.authorDutta Gupta, S.
dc.contributor.authorChui, W.
dc.date.accessioned2017-01-30T13:37:57Z
dc.date.available2017-01-30T13:37:57Z
dc.date.created2015-10-29T04:08:52Z
dc.date.issued2013
dc.identifier.citationBera, 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.
dc.identifier.urihttp://hdl.handle.net/20.500.11937/33573
dc.identifier.doi10.1111/cbdd.12171
dc.description.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.

dc.titleSynthesis and in vitro evaluation of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives as thymidine phosphorylase inhibitors
dc.typeJournal Article
dcterms.source.volume82
dcterms.source.number3
dcterms.source.startPage351
dcterms.source.endPage360
dcterms.source.issn1747-0277
dcterms.source.titleChemical Biology and Drug Design
curtin.departmentSchool of Pharmacy
curtin.accessStatusFulltext not available


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