Synthesis and in vitro evaluation of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives as thymidine phosphorylase inhibitors
dc.contributor.author | Bera, H. | |
dc.contributor.author | Dolzhenko, Anton | |
dc.contributor.author | Sun, L. | |
dc.contributor.author | Dutta Gupta, S. | |
dc.contributor.author | Chui, W. | |
dc.date.accessioned | 2017-01-30T13:37:57Z | |
dc.date.available | 2017-01-30T13:37:57Z | |
dc.date.created | 2015-10-29T04:08:52Z | |
dc.date.issued | 2013 | |
dc.identifier.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. | |
dc.identifier.uri | http://hdl.handle.net/20.500.11937/33573 | |
dc.identifier.doi | 10.1111/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.title | Synthesis and in vitro evaluation of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives as thymidine phosphorylase inhibitors | |
dc.type | Journal Article | |
dcterms.source.volume | 82 | |
dcterms.source.number | 3 | |
dcterms.source.startPage | 351 | |
dcterms.source.endPage | 360 | |
dcterms.source.issn | 1747-0277 | |
dcterms.source.title | Chemical Biology and Drug Design | |
curtin.department | School of Pharmacy | |
curtin.accessStatus | Fulltext not available |
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