Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents

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YURTTAŞ L., Şahin Z., Çiftçi G. A., TEMEL H. E., Demirayak Ş.

Acta Pharmaceutica Sciencia, vol.54, no.1, pp.83-92, 2016 (Scopus) identifier

  • Publication Type: Article / Article
  • Volume: 54 Issue: 1
  • Publication Date: 2016
  • Doi Number: 10.23893/1307-2080.aps.0547
  • Journal Name: Acta Pharmaceutica Sciencia
  • Journal Indexes: Scopus
  • Page Numbers: pp.83-92
  • Keywords: Antitumor, Cytotoxicity, Lipooxygenase (LOX) inhibition, Triazine
  • Istanbul Medipol University Affiliated: Yes


In this study, new 3, 5, 6-trisubstituted 1, 2, 4-triazine derivatives (1-9) were synthesized and their structures were determined by using NMR, IR and Mass spectroscopic methods. In vitro antitumor activities against MCF-7 breast adenocarcinoma and C6 rat glioma cell lines were evaluated via MTT colorimetric assay. Among the compounds, compound 4 (IC50=21.0 µg/mL) was found as the most active one against C6 cell line, whereas compound 5 (IC50=9.5 µg/mL) was found the most potent compound against MCF-7 cell line and both of compounds had higher activity than cisplatin in their line. Furthermore, IC50 value of compound 6 was found as 26.0 µg/mL against C6 which was very close to cisplatin potency (IC50=23.5 µg/mL). Besides, all compounds were tested to determine their lipoxygenase (LOX) inhibitory activity. Compounds 1 and 6 showed LOX inhibition with percentages of 43.35% and 38.79% at 100 µg/mL concentration, respectively. The obtained results on cell lines inspire to synthesise new and more potent molecules compounds as anticancer agents.