Discovery of ‘click’ 1,2,3-triazolium salts as potential anticancer drugs
Article Category: Research Article
Published Online: Jul 19, 2016
Page range: 280 - 288
Received: Nov 23, 2015
Accepted: Mar 17, 2016
DOI: https://doi.org/10.1515/raon-2016-0027
© Radiol Oncol 2016
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Background
In order to increase the effectiveness of cancer treatment, new compounds with potential anticancer activities are synthesized and screened. Here we present the screening of a new class of compounds, 1-(2-picolyl)-, 4-(2-picolyl)-, 1-(2-pyridyl)-, and 4-(2-pyridyl)-3-methyl-1,2,3-triazolium salts and ‘parent’ 1,2,3-triazole precursors.
Methods
Cytotoxic activity of new compounds was determined by spectrophotometric MTT assay on several tumour and one normal cell line. Effect of the selected compound to bind double stranded DNA (ds DNA) was examined by testing its influence on thermal stability of calf thymus DNA while its influence on cell cycle was determined by flow cytometric analysis. Generation of reactive oxygen species (ROS) was determined by addition of specific substrate 5-(and-6)-chloromethyl-2’,7’-dichlorodihydrofluorescein diacetate, acetyl ester (CM-H2DCFDA).
Results
Parent triazoles were largely inactive, while some of the triazolium salts were highly cytotoxic for HeLa cells. Triazolium salts exhibited high cell-type dependent cytotoxicity against different tumour cells. Selected compound (4-(4-methoxyphenyl)-3-methyl-1-(2-picolyl)-1
Conclusions
Our results suggest that the ‘click’ triazolium salts are worthy of further investigation as anti-cancer agents.