Biopolym. Cell. 2021; 37(4):303-314.
Bioorganic Chemistry
Evaluation of the antiproliferative activity of selected 1,2,3-triazole-4-carboxylic acids — key fragments and precursors of antitumor 1,2,3-triazole-4-carboxamides
1Pokhodylo N. T., 1Matiychuk V. S.
  1. Ivan Franko National University of Lviv
    4, Hrushevskoho Str., Lviv, Ukraine, 79005


Aim. To evaluate in vitro antiproliferative effect of selected 1,2,3-triazole-4-carboxylic acids, which are the key fragments and precursors of antitumor 1,2,3-triazole-4-carboxamides. Methods. Organic synthesis, in vitro cytotoxicity assay, MTT assay, spectrophotometry, statistical analysis. Results. The selected 1,2,3-triazole carboxylic acids and their esters synthesized according to a convenient synthetic procedure were tested for their anticancer activity in NCI60 cell lines within 9 cancer types at the 60 human tumour cell lines panel. These preliminary results allowed identifying the most active compounds and finding the structure-activity relations. The most promising 1,2,3-triazole-4-carboxylic fragments were selected for the design of 1,2,3-triazole-4-carboxamides for screening anticancer activity. Conclusions. The obtained results of antitumour activity of the studied derivatives are interesting for the discovery of selective and active anticancer agents among 1,2,3-triazole-4-carboxamides in terms of a fragment-based drug discovery (FBDD) concept, that proves the necessity of further studies.
Keywords: 1,2,3-triazoles, 1,2,3-triazole-4-carboxamides, 1,2,3-triazole-4-carboxylic acids, anticancer activity, cell proliferation


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