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

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, sta-tistical 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 rela-tions. 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.