Biopolym. Cell. 2021; 37(4):303-314.
http://dx.doi.org/10.7124/bc.000A5C
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

Abstract

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
Full text: (PDF, in English)

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